The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28039836 |
41 |
Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities. |
East China Normal University |
| 28006668 |
1 |
Design and synthesis of novel 7-aminosubstituted pyrido[2,3-b]pyrazines exhibiting anti-breast cancer activity. |
Biomedical Research Foundation Academy of Athens (Brfaa) |
| 28108251 |
50 |
Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kd inhibitors. |
Bristol-Myers Squibb |
| 28129991 |
2 |
Identification of allosteric binding sites for PI3Ka oncogenic mutant specific inhibitor design. |
Johns Hopkins University School of Medicine |
| 28280261 |
84 |
Non-kinase targets of protein kinase inhibitors. |
The University of Sydney |
| 27479483 |
61 |
6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors. |
Csir-Indian Institute of Integrative Medicine |
| 27816514 |
103 |
Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties. |
Novartis Institutes For Biomedical Research |
| 27448924 |
53 |
Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor. |
Second Military Medical University |
| 27994725 |
107 |
Imidazopyridazine Inhibitors of PI3Kß. |
Dart Neuroscience |
| 27765510 |
8 |
Synthesis of linear and angular aryl-morpholino-naphth-oxazines, their DNA-PK, PI3K, PDE3A and antiplatelet activity. |
La Trobe University |
| 28004945 |
52 |
Rational Design of Novel Highly Potent and Selective Phosphatidylinositol 4-Kinase IIIß (PI4KB) Inhibitors as Broad-Spectrum Antiviral Agents and Tools for Chemical Biology. |
Academy of Sciences of The Czech Republic |
| 27644332 |
59 |
Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
Curtin University |
| 27575470 |
12 |
Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors. |
Novartis Institutes For Biomedical Research |
| 27171036 |
164 |
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
University of Nebraska Medical Center |
| 27774129 |
2 |
Concise SAR Exploration Based on the"Head-to-Tail" Approach: Discovery of PI4KIIIa Inhibitors Bearing Diverse Scaffolds. |
Japan Tobacco |
| 27774127 |
75 |
Discovery of a Series of 5,11-Dihydro-6 |
Dana-Farber Cancer Institute |
| 27660692 |
70 |
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-¿ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate. |
Infinity Pharmaceuticals |
| 27353887 |
9 |
Synthesis and anticancer activity of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives bearing chromone moiety. |
Jiangxi Science & Technology Normal University |
| 27217002 |
96 |
Discovery of novel 7-azaindoles as PDK1 inhibitors. |
Merck |
| 27096040 |
17 |
Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR. |
Genentech |
| 27089211 |
38 |
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors. |
Zhejiang University |
| 27117263 |
51 |
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors. |
Takeda Pharmaceutical |
| 27084677 |
16 |
Computer-aided design, synthesis, and biological evaluation of new indole-2-carboxamide derivatives as PI3Ka/EGFR inhibitors. |
The University of Jordan |
| 27043268 |
16 |
Design, synthesis, biological evaluation and docking studies of novel 2-substituted-4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as dual PI3Ka/mTOR inhibitors. |
Jiangxi Science & Technology Normal University |
| 26885694 |
34 |
Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIß. |
University of California |
| 26951750 |
59 |
Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors. |
Novartis Institutes For Biomedical Research |
| 26951753 |
336 |
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors. |
Novartis Institutes For Biomedical Research |
| 26819669 |
39 |
Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo. |
Novartis Institutes For Biomedical Research |
| 26896709 |
113 |
Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2. |
Saarland University |
| 26713102 |
36 |
Discovery of Novel and Orally Bioavailable Inhibitors of PI3 Kinase Based on Indazole Substituted Morpholino-Triazines. |
Sphaera Pharma |
| 26741947 |
24 |
The Rational Design of Selective Benzoxazepin Inhibitors of thea-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326). |
Genentech |
| 26731167 |
32 |
Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents. |
Sun Yat-Sen University |
| 26854431 |
47 |
Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines. |
La Trobe University |
| 26819001 |
29 |
Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. |
Second Military Medical University |
| 26774655 |
32 |
Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model. |
Novartis Institutes For Biomedical Research |
| 26086931 |
38 |
Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators. |
Shandong University |
| 26298499 |
47 |
The imidazo[1,2-a]pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors. |
Amgen |
| 26349627 |
133 |
Discovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9. |
The University of Melbourne |
| 26164189 |
21 |
Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Ka inhibitor with high PI3K isoform selectivity and potent cellular activity. |
Novartis Institutes For Biomedical Research |
| 26119500 |
22 |
Discovery of a 6-(pyridin-3-yl)benzo[d]thiazole template for optimization of hedgehog and PI3K/AKT/mTOR dual inhibitors. |
Soochow University |
| 26199119 |
135 |
Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors. |
Novartis Institutes For Biomedical Research |
| 26210161 |
15 |
Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea. |
Xi'An Jiaotong University |
| 26112437 |
20 |
Synthesis and evaluation of pyrrolotriazine based molecules as PI3 kinase inhibitors. |
Sphaera Pharma |
| 26099539 |
18 |
Molecular modeling based approach, synthesis, and cytotoxic activity of novel benzoin derivatives targeting phosphoinostide 3-kinase (PI3Ka). |
Al-Zaytoonah University of Jordan |
| 26087940 |
287 |
Discovery of potent, selective small molecule inhibitors ofa-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIa). |
Astrazeneca |
| 25980912 |
41 |
Design of selective PI3Ka inhibitors starting from a promiscuous pan kinase scaffold. |
Astrazeneca |
| 25890698 |
135 |
Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling. |
University of Auckland |
| 26121481 |
37 |
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿. |
Vertex Pharmaceuticals |
| 26102506 |
40 |
Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
Celgene |
| 26083478 |
66 |
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
Celgene |
| 26005528 |
41 |
Discovery of a Potent Class of PI3Ka Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT). |
Glaxosmithkline |
| 25893045 |
44 |
Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors. |
Pkucare Pharmaceutical R & D Center |
| 25835317 |
63 |
Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
Sichuan University |
| 25911625 |
1 |
Synthesis and antitumor activities evaluation of m-(4-morpholinoquinazolin-2-yl)benzamides in vitro and in vivo. |
Xi'An Jiaotong University |
| 25659752 |
16 |
Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Ka inhibitors. |
Jiangxi Science & Technology Normal University |
| 25643210 |
16 |
Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2. |
Astrazeneca |
| 25514658 |
182 |
Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3Kß and PI3Kd for the treatment of PTEN-deficient cancers. |
Astrazeneca |
| 25827523 |
275 |
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors. |
Vertex Pharmaceuticals |
| 25765909 |
1 |
Design, synthesis and antiproliferative activity evaluation of m-(4-morpholinyl-1,3,5-triazin-2-yl)benzamides in vitro. |
Xi'An Jiaotong University |
| 25693787 |
44 |
6,7-Dihydrobenzo[f]benzo[4,5]imidazo[1,2-d][1,4]oxazepine derivatives as selective inhibitors of PI3Ka. |
Nanjing University |
| 25666823 |
90 |
Synthesis and SAR study of potent and selective PI3Kd inhibitors. |
Amgen |
| 25387153 |
53 |
Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring. |
University Hospital Hradec Kralove |
| 25139570 |
31 |
Synthesis and structure-activity relationships of PI3K/mTOR dual inhibitors from a series of 2-amino-4-methylpyrido[2,3-d]pyrimidine derivatives. |
Pkucare Pharmaceutical R & D Center |
| 25086238 |
13 |
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents. |
Shenyang Pharmaceutical University |
| 25004409 |
79 |
Development and biological evaluation of potent and selective c-KIT(D816V) inhibitors. |
Korea Advanced Institute of Science and Technology (Kaist) |
| 25042253 |
52 |
Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kß inhibitors, useful as antiplatelet agents. |
Astrazeneca |
| 24992874 |
58 |
Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kß/d inhibitors for the treatment of PTEN-deficient tumours. |
Astrazeneca |
| 24754609 |
35 |
Structural basis for isoform selectivity in a class of benzothiazole inhibitors of phosphoinositide 3-kinase¿. |
Vertex Pharmaceuticals |
| 25589928 |
37 |
Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors. |
Novartis Institutes For Biomedical Research |
| 25589927 |
36 |
Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors. |
Novartis Institutes For Biomedical Research |
| 25589920 |
72 |
Quinalozinones as Inhibitors of Class I PI3K Kinases. |
Dart Neuroscience |
| 25589915 |
41 |
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
Monash University (Parkville Campus) |
| 25468038 |
8 |
Design, synthesis, anticancer activity and docking studies of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as mTOR inhibitors. |
TBA |
| 25440879 |
13 |
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents. |
Shenyang Pharmaceutical University |
| 25248682 |
18 |
Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors. |
Universit£ |
| 24805946 |
25 |
Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
Northeastern University |
| 24773549 |
20 |
Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties. |
Development Center For Biotechnology |
| 24560540 |
119 |
Preparation and optimization of new 4-(2-(indolin-1-yl)-2-oxoethyl)-2-morpholinothiazole-5-carboxylic acid and amide derivatives as potent and selective PI3Kß inhibitors. |
Sanofi |
| 24433860 |
60 |
Identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors. |
Pkucare Pharmaceutical R & D Center |
| 24387221 |
150 |
Discovery and optimization of pyrimidone indoline amide PI3Kß inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers. |
Sanofi |
| 24900786 |
9 |
Crystal Structures of PI3K? Complexed with PI103 and Its Derivatives: New Directions for Inhibitors Design. |
Shanghai Jiao Tong University |
| 23855836 |
147 |
1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity. |
Newcastle University |
| 23820386 |
32 |
Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K. |
Novartis Institutes For Biomedical Research |
| 23932790 |
73 |
A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors. |
Genentech |
| 23867164 |
27 |
Identification of GNE-293, a potent and selective PI3Kd inhibitor: navigating in vitro genotoxicity while improving potency and selectivity. |
Genentech |
| 23726034 |
117 |
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. |
Novartis Institutes For Biomedical Research |
| 23662903 |
34 |
Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): aß-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. |
Genentech |
| 23540645 |
140 |
Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinaseß isoform. |
Genentech |
| 23414803 |
9 |
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase. |
Celgene |
| 23394126 |
170 |
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR). |
Exelixis |
| 23375793 |
26 |
Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014. |
Astrazeneca |
| 24900568 |
27 |
Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design. |
Pfizer |
| 23410005 |
147 |
Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors. |
The University of Arizona |
| 23394205 |
106 |
Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. |
Astrazeneca |
| 23265896 |
36 |
Regioselective synthesis of 5- and 6-methoxybenzimidazole-1,3,5-triazines as inhibitors of phosphoinositide 3-kinase. |
Monash Institute of Pharmaceutical Sciences |
| 23265894 |
40 |
Cis-amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase. |
Genentech |
| 23795239 |
62 |
L-Aminoacyl-triazine derivatives are isoform-selective PI3K? inhibitors that target non-conserved Asp862 of PI3K? |
Monash University (Parkville Campus) |
| 23360348 |
11 |
Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Ka. |
Celgene Avilomics Research |
| 23265889 |
31 |
Lead optimization of a dihydropyrrolopyrimidine inhibitor against phosphoinositide 3-kinase (PI3K) to improve the phenol glucuronic acid conjugation. |
Chugai Pharmaceutical |
| 22520259 |
65 |
Identification of ETP-46321, a potent and orally bioavailable PI3Ka,d inhibitor. |
Spanish National Cancer Research Centre (Cnio) |
| 24900504 |
107 |
Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors. |
TBA |
| 22924688 |
128 |
PI3Kd and PI3K¿ as targets for autoimmune and inflammatory diseases. |
Amgen |
| 23122859 |
43 |
Discovery and optimization of a series of 2-aminothiazole-oxazoles as potent phosphoinositide 3-kinase¿ inhibitors. |
Taisho Pharmaceutical |
| 23059543 |
39 |
Synthesis, DNA-PK inhibition, anti-platelet activity studies of 2-(N-substituted-3-aminopyridine)-substituted-1,3-benzoxazines and DNA-PK and PI3K inhibition, homology modelling studies of 2-morpholino-(7,8-di and 8-substituted)-1,3-benzoxazines. |
La Trobe University |
| 22832322 |
40 |
Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold. |
Amgen |
| 22726925 |
216 |
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease. |
Cellzome |
| 22946614 |
9 |
The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinasea. |
Genentech |
| 23063403 |
21 |
Recent results in protein kinase inhibition for tropical diseases. |
Montclair State University |
| 22877085 |
33 |
Potent and highly selective benzimidazole inhibitors of PI3-kinase delta. |
Genentech |
| 22876881 |
72 |
Discovery and in vivo evaluation of dual PI3Kß/d inhibitors. |
Amgen |
| 22765895 |
72 |
Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors. |
Amgen |
| 23010262 |
46 |
Discovery of phosphoinositide 3-kinases (PI3K) p110ß isoform inhibitor 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2-methylmorpholin-4-yl]-1H-pyrimidin-2-one, an effective antithrombotic agent without associated bleeding and insulin resistance. |
Astrazeneca |
| 22548365 |
293 |
Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases. |
Amgen |
| 23021994 |
108 |
Identification of pyrimidine derivatives as hSMG-1 inhibitors. |
Pfizer |
| 23010274 |
48 |
Discovery of 4-morpholino-pyrimidin-6-one and 4-morpholino-pyrimidin-2-one-containing Phosphoinositide 3-kinase (PI3K) p110ß isoform inhibitors through structure-based fragment optimisation. |
Astrazeneca |
| 22548342 |
210 |
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors. |
Exelixis |
| 22981333 |
103 |
Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3Kß inhibitors. |
Sanofi |
| 22575050 |
40 |
Design, synthesis, and evaluation of 3,5-disubstituted 7-azaindoles as Trk inhibitors with anticancer and antiangiogenic activities. |
Korea Advanced Institute of Science and Technology (Kaist) |
| 23063566 |
70 |
Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Ka inhibitors. |
Universit£ |
| 22863202 |
94 |
Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway. |
Novartis Institutes For Biomedical Research |
| 22819766 |
173 |
SAR studies around a series of triazolopyridines as potent and selective PI3K¿ inhibitors. |
Cellzome |
| 22765900 |
24 |
Conformationally-restricted cyclic sulfones as potent and selective mTOR kinase inhibitors. |
Pfizer |
| 22524426 |
281 |
Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kß inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers. |
Sanofi Research & Development |
| 22819764 |
35 |
Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR. |
Spanish National Cancer Research Centre (Cnio) |
| 22771009 |
9 |
Discovery of MEK/PI3K dual inhibitor via structure-based virtual screening. |
Sejong University |
| 22738635 |
87 |
Discovery of novel PI3K¿/d inhibitors as potential agents for inflammation. |
Cellzome |
| 22738630 |
76 |
Structure-based optimization of aminopyridines as PKC¿ inhibitors. |
Vertex Pharmaceuticals |
| 22607682 |
47 |
Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor. |
Astrazeneca |
| 22168626 |
32 |
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E. |
Ambit Biosciences |
| 22480851 |
6 |
Discovery of novel 2-piperidinol-3-(arylsulfonyl)quinoxalines as phosphoinositide 3-kinasea (PI3Ka) inhibitors. |
Zhejiang University |
| 22475557 |
75 |
Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potentß isoform selective phosphatidylinositol 3-kinase inhibitors. |
Glaxosmithkline |
| 24900266 |
24 |
Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer. |
TBA |
| 24900269 |
18 |
Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity. |
TBA |
| 21067921 |
13 |
Discovery of new azaindole-based PI3Ka inhibitors: apoptotic and antiangiogenic effect on cancer cells. |
Institute of Science and Technology (Kaist) |
| 20166697 |
71 |
Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. |
Wyeth Research |
| 18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 19081716 |
57 |
Optimization of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine inhibitors of IGF-1R: elimination of an acid-mediated decomposition pathway. |
Glaxosmithkline |
| 19297156 |
43 |
Exploring the PI3K alpha and gamma binding sites with 2,6-disubstituted isonicotinic derivatives. |
University of Cincinnati |
| 14593182 |
34 |
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. |
Pfizer |
| 18501601 |
1 |
Design and synthesis of novel furoquinoline based inhibitors of multiple targets in the PI3K/Akt-mTOR pathway. |
Nicholas Piramal Research Centre |
| 18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
| 18248814 |
24 |
Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway. |
Novartis Institute For Biomedical Research |
| 17339109 |
33 |
Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors. |
Astellas Pharma |
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Synthesis and structure-activity relationships of imidazo[1,2-a]pyrimidin-5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors. |
Glaxosmithkline |
| 22336246 |
7 |
JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
Tianjin Key Laboratory On Technologies Enabling Development of Clinical Therapeutics and Diagnostics |
| 21985639 |
70 |
Rational design of phosphoinositide 3-kinasea inhibitors that exhibit selectivity over the phosphoinositide 3-kinaseß isoform. |
Genentech |
| 22136433 |
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7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes. |
Ludwig-Maximilians University of Munich |
| 21978683 |
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Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2-ones as potent and selective mTOR kinase inhibitors. |
Celgene |
| 22197143 |
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Structure-based optimization of morpholino-triazines as PI3K and mTOR inhibitors. |
S*Bio |
| 22130133 |
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Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
Chinese Academy of Sciences |
| 22177407 |
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Novel pyrazolo[1,5-a]pyridines as p110a-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR. |
University of Auckland |
| 22177405 |
104 |
Discovery of pyrazolo[1,5-a]pyridines as p110a-selective PI3 kinase inhibitors. |
University of Auckland |
| 22030027 |
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Discovery of new aminopyrimidine-based phosphoinositide 3-kinase beta (PI3Kß) inhibitors with selectivity over PI3Ka. |
Institute of Science and Technology (Kaist) |
| 21981714 |
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Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. |
Genentech |
| 22014755 |
36 |
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. |
Hanyang University |
| 21612232 |
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Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives. |
Amgen |
| 21925880 |
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Fragment based discovery of a novel and selective PI3 kinase inhibitor. |
Pfizer |
| 21882832 |
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Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474). |
University of Auckland |
| 22037378 |
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Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
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Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl)quinoxalines as PI3Ka inhibitors. |
Zhejiang University |
| 21936542 |
143 |
Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. |
Novartis Institute For Biomedical Research |
| 21714526 |
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Structure-activity relationships of phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: investigations of various 6,5-heterocycles to improve metabolic stability. |
Amgen |
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Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors. |
Pfizer |
| 20561789 |
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Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment. |
Sanofi-Aventis |
| 21636270 |
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Structure-based design of thienobenzoxepin inhibitors of PI3-kinase. |
Genentech |
| 21332118 |
157 |
Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors. |
Amgen |
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22 |
Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis. |
Korea Advanced Institute of Science and Technology |
| 21322566 |
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Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer. |
Dana-Farber Cancer Institute |
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Discovery of triazine-benzimidazoles as selective inhibitors of mTOR. |
Amgen |
| 21354792 |
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Structure-based virtual screening approach to the discovery of phosphoinositide 3-kinase alpha inhibitors. |
Sejong University |
| 24900229 |
41 |
Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery. |
TBA |
| 21316229 |
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Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. |
Chugai Pharmaceutical |
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Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase Inhibitors |
TBA |
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Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors. |
Pfizer |
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DNA-dependent protein kinase (DNA-PK) inhibitors: structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain. |
Newcastle University |
| 21216151 |
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Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements. |
The Institute of Cancer Research |
| 21169017 |
63 |
Discovery of novel class 1 phosphatidylinositide 3-kinases (PI3K) fragment inhibitors through structure-based virtual screening. |
Astrazeneca R & D M£Lndal |
| 21062009 |
70 |
Design, Synthesis, and Structure−Activity Relationships of 3-Ethynyl-1H-indazoles as Inhibitors of the Phosphatidylinositol 3-Kinase Signaling Pathway |
TBA |
| 21121631 |
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Synthesis of phosphatidylinositol 3-kinase (PI3K) inhibitory analogues of the sponge meroterpenoid liphagal. |
University of British Columbia |
| 21035331 |
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Identification and structure-activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors. |
Novartis Institutes For Biomedical Research |
| 20860370 |
83 |
Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. |
Dana-Farber Cancer Institute |
| 20822905 |
28 |
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase. |
Genentech |
| 20797855 |
63 |
PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor. |
Pfizer |
| 19654408 |
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AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
| 20081827 |
52 |
The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors. |
Medical Research Council-Laboratory of Molecular Biology |
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5-ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-alpha and mTOR for the treatment of breast cancer. |
Wyeth Research |
| 19894727 |
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Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent. |
Wyeth Research |
| 20346656 |
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Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor. |
Genentech |
| 20334367 |
78 |
Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors. |
Wyeth Research |
| 20307980 |
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B-Raf kinase inhibitors: hit enrichment through scaffold hopping. |
Wyeth Research |
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Novel benzofuran-3-one indole inhibitors of PI3 kinase-alpha and the mammalian target of rapamycin: hit to lead studies. |
Wyeth Research |
| 20223664 |
36 |
Triazines incorporating (R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kalpha. |
Wyeth Research |
| 20223663 |
100 |
2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability. |
Wyeth Research |
| 20188552 |
75 |
Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). |
Wyeth Research |
| 20188551 |
56 |
4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). |
Wyeth Research |
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47 |
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors. |
Wyeth Research |
| 20166671 |
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Selectively nonselective kinase inhibition: striking the right balance. |
Schering-Plough |
| 20050669 |
61 |
Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer. |
Genentech |
| 19864136 |
45 |
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors. |
Wyeth Research |
| 19762236 |
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The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase. |
Kudos Pharmaceuticals |
| 19968288 |
83 |
Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402. |
Wyeth Research |
| 20089401 |
46 |
Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 1-substituent. |
Wyeth Research |
| 19969455 |
70 |
Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies. |
Wyeth Research |
| 19963384 |
26 |
Discovery of 3,6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d]pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). |
Wyeth Research |
| 19954970 |
64 |
Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors. |
Wyeth Research |
| 19897362 |
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Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K. |
Wyeth Research |
| 19896845 |
54 |
Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: discovery of highly potent and selective analogs with improved human microsomal stability. |
Wyeth Research |
| 19733066 |
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Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR. |
Kudos Pharmaceuticals |
| 19916508 |
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Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors. |
Wyeth Research |
| 19523825 |
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A stabilized demethoxyviridin derivative inhibits PI3 kinase. |
Harvard Medical School |
| 19362830 |
47 |
Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors. |
Wyeth Research |
| 18815050 |
34 |
4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors. |
Wyeth Research |
| 18774713 |
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Optimization of a series of multi-isoform PI3 kinase inhibitors. |
Ucb Pharma |
| 18682324 |
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Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors. |
Amgen |
| 18644721 |
131 |
Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines. |
Ucb Pharma |
| 18630894 |
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Slow self-activation enhances the potency of viridin prodrugs. |
Harvard Medical School |
| 18625552 |
88 |
4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase. |
Ucb Pharma |
| 17869522 |
51 |
Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors. |
University of Auckland |
| 16789742 |
65 |
Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma. |
Serono Pharmaceutical Research Institute |
| 15658870 |
104 |
Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro. |
Newcastle University |
| 15546735 |
25 |
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries. |
University of Newcastle |
| 32676155 |
54 |
Discovery of 3-Quinazolin-4(3 |
Luoxin Pharmaceutical (Shanghai) Co. |
| 32676144 |
34 |
Design and Development of a Macrocyclic Series Targeting Phosphoinositide 3-Kinase ?. |
Gsk Medicines Research Centre |
| 32435375 |
22 |
New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
Universidad San Pablo-Ceu |
| 31787462 |
4 |
Pyrazolopyrimide library screening in glioma cells discovers highly potent antiproliferative leads that target the PI3K/mTOR pathway. |
University of Edinburgh |
| 31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
| 27544401 |
10 |
Synthesis and antitumor activity evaluation of 4,6-disubstituted quinazoline derivatives as novel PI3K inhibitors. |
Xi'An Jiaotong University |
| 27429068 |
54 |
Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
Glaxosmithkline R&D |
| 27259031 |
191 |
Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase. |
Astrazeneca |
| 27561716 |
95 |
Development of single and mixed isoform selectivity PI3K? inhibitors by targeting Asn836 of PI3K?. |
Monash University |
| 27563400 |
133 |
Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors. |
Novartis Institutes For Biomedical Research |
| 30605829 |
24 |
Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3K?. |
China Pharmaceutical University |
| 31647659 |
576 |
Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of |
University of Nottingham |
| 31749911 |
68 |
Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors. |
Nestl� |
| 31749910 |
26 |
INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3K?). |
Incyte |
| 32212730 |
206 |
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
National Center For Advancing Translational Sciences |
| 31851518 |
61 |
The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5- |
Astrazeneca |
| 31434616 |
32 |
Synthesis and biological evaluation of 4-(piperid-3-yl)amino substituted 6-pyridylquinazolines as potent PI3K? inhibitors. |
Xi'An Jiaotong University |
| 30582807 |
22 |
Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective. |
University Park Nottingham |
| 30532965 |
81 |
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach. |
Glaxosmithkline R&D |
| 31955578 |
37 |
Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders. |
Novartis Institutes For Biomedical Research |
| 31846325 |
46 |
Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy. |
TBA |
| 31581005 |
29 |
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer. |
Ain Shams University |
| 31381325 |
46 |
Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents. |
Chengdu University |
| 30755348 |
45 |
Optimization of 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidines to generate a highly selective PI3K? inhibitor. |
Astellas Pharma |
| 31543303 |
17 |
Rational discovery of a highly novel and selective mTOR inhibitor. |
Takeda California |
| 31446244 |
70 |
Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3K?. |
School of Traditional Chinese Pharmacy |
| 31244112 |
46 |
( |
University of Basel |
| 31029551 |
64 |
Design, synthesis and biological evaluation of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates containing sulfonamido as potential PI3K? inhibitors. |
School of Traditional Chinese Pharmacy |
| 30530193 |
64 |
Targeting the immunity protein kinases for immuno-oncology. |
China Pharmaceutical University |
| 31855425 |
224 |
Optimization of Orally Bioavailable PI3K? Inhibitors and Identification of Vps34 as a Key Selectivity Target. |
Glaxosmithkline |
| 31465220 |
139 |
A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor. |
University of Basel |
| 31283227 |
72 |
Discovery of 3-Oxabicyclo[4.1.0]heptane, a Non-nitrogen Containing Morpholine Isostere, and Its Application in Novel Inhibitors of the PI3K-AKT-mTOR Pathway. |
Glaxosmithkline R&D |
| 31117517 |
103 |
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases. |
TBA |
| 29211480 |
64 |
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy. |
China Pharmaceutical University |
| 26996374 |
75 |
Discovery of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides as PI3K?/? inhibitors for the treatment of PTEN-deficient tumours. |
Astrazeneca |
| 26505898 |
123 |
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies. |
Novartis Institutes For Biomedical Research |
| 26613634 |
11 |
Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability. |
Chugai Pharmaceutical |
| 26596710 |
27 |
Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation. |
Zhejiang University |
| 26206504 |
131 |
Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors. |
Novartis Institutes For Biomedical Research |
| 24345273 |
111 |
Design, synthesis, and biological activity of pyridopyrimidine scaffolds as novel PI3K/mTOR dual inhibitors. |
Universit£ |
| 24900655 |
165 |
[3a,4]-Dihydropyrazolo[1,5a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase ? Inhibitors. |
Glaxosmithkline |
| 31176568 |
34 |
Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors. |
Xi'An Jiaotong University |
| 30359003 |
104 |
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
University of Basel |
| 30380865 |
19 |
Neolymphostin A Is a Covalent Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitor That Employs an Unusual Electrophilic Vinylogous Ester. |
University of California San Diego |
| 30346772 |
124 |
Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. |
Astrazeneca |
| 30245395 |
50 |
Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3K? H1047R mutant inhibitors. |
Chongqing University |
| 29541370 |
41 |
Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR. |
Wuxi Apptec (Shanghai) Co. |
| 30077608 |
24 |
Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3K?. |
China Pharmaceutical University |
| 29945756 |
29 |
Design and synthesis of alkyl substituted pyridino[2,3-D]pyrimidine compounds as PI3K?/mTOR dual inhibitors with improved pharmacokinetic properties and potent in vivo antitumor activity. |
Nanjing University of Chinese Medicine |
| 29937355 |
8 |
Design, synthesis and biological evaluation of novel series of 2H-benzo[b][1,4]oxazin-3(4H)-one and 2H-benzo[b][1,4]oxazine scaffold derivatives as PI3K? inhibitors. |
Shenyang Pharmaceutical University |
| 29601991 |
22 |
Discovery of novel quinazolinone derivatives as high potent and selective PI3K? and PI3K?/? inhibitors. |
Shandong University |
| 29631787 |
21 |
Discovery and biological evaluation of novel pyrazolopyridine derivatives as potent and orally available PI3K? inhibitors. |
Astellas Pharma |
| 29559278 |
99 |
Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases. |
Astrazeneca |
| 29534936 |
30 |
Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3K?) inhibitors. |
Xi'An Jiaotong University |
| 29486969 |
14 |
Design and synthesis of 1,4-substituted 1H-1,2,3-triazolo-quinazolin-4(3H)-ones by Huisgen 1,3-dipolar cycloaddition with PI3K? isoform selective activity. |
India Academy of Scientific & Innovative Research (Acsir) |
| 29305298 |
28 |
Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors. |
Chinese Academy of Medical Sciences and Peking Union Medical College |
| 30128072 |
68 |
Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors. |
Astrazeneca |
| 30034607 |
60 |
Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines. |
Shanghai Haiyan Pharmaceutical Technology |
| 29407971 |
15 |
Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3K?. |
Shenyang Pharmaceutical University |
| 30053721 |
184 |
Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3K?) inhibitor. |
Chinese Academy of Sciences |
| 29683659 |
127 |
The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one). |
Astrazeneca |
| 29625382 |
8 |
Phthalimide conjugations for the degradation of oncogenic PI3K. |
Tsinghua University |
| 29927604 |
90 |
Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment. |
Chinese Academy of Medical Sciences and Peking Union Medical College |
| 29057057 |
54 |
From PIM1 to PI3K? via GSK3?: Target Hopping through the Kinome. |
Glaxosmithkline |
| 28947947 |
112 |
Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors. |
Novartis Institutes For Biomedical Research |
| 29852070 |
101 |
Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-? Inhibitors. |
Pharmaron-Beijing |
| 28835793 |
32 |
Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168). |
University of Michigan |
| 28835784 |
77 |
Potential of PI3K? Inhibitors in the Treatment of Cancer and Other Diseases. |
Therachem Research Medilab (India) |
| 28633896 |
13 |
Design, synthesis and biological evaluation of novel 3H-imidazole [4,5-b] pyridine derivatives as selective mTOR inhibitors. |
China Pharmaceutical University |
| 28128944 |
96 |
Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase? (PI3K?) Inhibitors. |
University Park Nottingham |
| 28259529 |
31 |
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
The Ohio State University |
| 27846451 |
60 |
SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3K?) inhibitors. |
Shanghai Institute of Materia Medica (Simm) |
| 28526367 |
30 |
Discovery of a novel aminopyrazine series as selective PI3K? inhibitors. |
Astrazeneca |
| 28341403 |
57 |
Thiazolidine derivatives as potent and selective inhibitors of the PIM kinase family. |
University of Oxford |
| 28462836 |
4 |
Iodine catalyzed three component synthesis of 1-((2-hydroxy naphthalen-1-yl)(phenyl)(methyl))pyrrolidin-2-one derivatives: Rationale as potent PI3K inhibitors and anticancer agents. |
Vit University |
| 28209465 |
124 |
Identification of highly potent and selective PI3K? inhibitors. |
Bristol-Myers Squibb |
| 28829592 |
109 |
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. |
University of Basel |
| 28541707 |
119 |
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase? (PI3K?) Inhibitor for the Treatment of Immunological Disorders. |
Bristol-Myers Squibb |
| 28347666 |
45 |
Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3K?/? inhibitors for the treatment of PTEN-deficient tumours. |
Astrazeneca |
| 22957724 |
30 |
Synthesis and characterization of metal complexes of heterocyclic sulfonamide as carbonic anhydrase inhibitors. |
Dumlupinar University |
| 22188522 |
45 |
Sulfapyridine-like benzenesulfonamide derivatives as inhibitors of carbonic anhydrase isoenzymes I, II and VI. |
Ataturk University |
| 21635211 |
12 |
Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols including natural products. |
Atatürk University |
| 20030517 |
18 |
Synthesis and activity of amides of tripeptides as potential urokinase inhibitors. |
Medical University of Bialystok |
| 20030504 |
38 |
Fluorobenzoyl dipeptidyl derivatives as inhibitors of the Fasciola hepatica cysteine protease cathepsin L1. |
Dublin City University |
| | 42 |
Ellagitannin and flavonoid constituents from Agrimonia pilosa Ledeb. with their protein tyrosine phosphatase and acetylcholinesterase inhibitory activities |
Catholic University of Daegu |
| | 15 |
Rational design, synthesis, pharmacophore modeling, and docking studies for identification of novel potent DNA-PK inhibitors |
Taibah University |
| 20879713 |
6 |
Kinetics and inhibition of nicotinamidase from Mycobacterium tuberculosis. |
Albert Einstein College of Medicine |
| 12815170 |
15 |
[125I]A-312110, a novel high-affinity 1,4-dihydropyridine ATP-sensitive K+ channel opener: characterization and pharmacology of binding. |
Abbott Laboratories |
| 12232544 |
79 |
[Second generation SSRIS: human monoamine transporter binding profile of escitalopram and R-fluoxetine]. |
Emory University |
| 9015795 |
50 |
Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors. |
University of Toronto |
| 6271132 |
14 |
Prostacyclin receptors of a neuronal hybrid cell line. Divalent citations and ligand-receptor coupling. |
Royal Postgraduate Medical School |
| 1325033 |
19 |
Receptor occupancy and adenylate cyclase activation in AR 4-2J rat pancreatic acinar cell membranes by analogs of pituitary adenylate cyclase-activating peptides amino-terminally shortened or modified at position 1, 2, 3, 20, or 21. |
Universit&Acute |
| 19090918 |
33 |
Inhibitors of tubulin assembly identified through screening a compound library. |
The Ohio State University |
| 16873019 |
6 |
MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells. |
Gpc Biotech |
| 15734645 |
4 |
Structural basis for the highly selective inhibition of MMP-13. |
Aventis Pharma Deutschland |
| 14741294 |
72 |
Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors. |
Merck Frosst Canada |
| 8027985 |
66 |
Tyrosine kinase inhibitors. 3. Structure-activity relationships for inhibition of protein tyrosine kinases by nuclear-substituted derivatives of 2,2'-dithiobis(1-methyl-N-phenyl-1H-indole-3-carboxamide). |
University of Auckland |
| 1552513 |
36 |
Inhibitors of protein kinase C. 2. Substituted bisindolylmaleimides with improved potency and selectivity. |
Roche Products |
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