The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28235701 |
10 |
Design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine derivatives as mTOR inhibitors. |
Peking University |
26652969 |
15 |
Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety. |
Xi'An Jiaotong University |
28109945 |
25 |
Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors. |
Hangzhou Xixi Hospital |
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 |
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 |
27644332 |
59 |
Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
Curtin University |
27115835 |
85 |
Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
University of Edinburgh |
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 |
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 |
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 |
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 |
26819001 |
29 |
Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. |
Second Military Medical University |
26318067 |
34 |
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
Hanyang University |
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 |
26321603 |
8 |
Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity. |
Xi'An Jiaotong University |
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 |
26162498 |
1 |
4-(N-Phenyl-N'-substituted benzenesulfonyl)-6-(4-hydroxyphenyl)quinolines as inhibitors of mammalian target of rapamycin. |
India Academy of Scientific & Innovative Research (Acsir) |
25980912 |
41 |
Design of selective PI3Ka inhibitors starting from a promiscuous pan kinase scaffold. |
Astrazeneca |
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 |
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 |
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 |
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 |
24893124 |
4 |
Development of synthetic lethality anticancer therapeutics. |
The University of Texas M.D. Anderson Cancer Center |
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 |
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 |
25466188 |
21 |
Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. |
Amgen |
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 |
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 |
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 |
24393580 |
6 |
Virtual screening and biochemical evaluation to identify new inhibitors of mammalian target of rapamycin (mTOR). |
Sejong University |
24387221 |
150 |
Discovery and optimization of pyrimidone indoline amide PI3Kß inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers. |
Sanofi |
24091081 |
49 |
Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach. |
Merck Research Laboratories |
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 |
23932790 |
73 |
A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors. |
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 |
23506825 |
71 |
Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series. |
Pfizer |
23414803 |
9 |
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase. |
Celgene |
23473235 |
21 |
Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR). |
Genentech |
23448267 |
17 |
Selective 3-phosphoinositide-dependent kinase 1 (PDK1) inhibitors: dissecting the function and pharmacology of PDK1. |
Glaxosmithkline |
23375793 |
26 |
Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014. |
Astrazeneca |
24900569 |
25 |
Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349. |
Genentech |
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 |
10843203 |
12 |
Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands. |
Glaxo Wellcome |
22520259 |
65 |
Identification of ETP-46321, a potent and orally bioavailable PI3Ka,d inhibitor. |
Spanish National Cancer Research Centre (Cnio) |
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 |
23199076 |
28 |
Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity. |
Genentech |
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 |
22897589 |
100 |
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
Amgen |
22765895 |
72 |
Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors. |
Amgen |
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 |
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 |
22863202 |
94 |
Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway. |
Novartis Institutes For Biomedical Research |
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) |
22749419 |
22 |
Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Ka and mTOR. |
Pfizer |
22607682 |
47 |
Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor. |
Astrazeneca |
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 |
21353571 |
26 |
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells. |
Hanyang University |
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 |
17350953 |
3 |
The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain. |
Stanford University |
16134928 |
34 |
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry. |
The Scripps Research Institute |
15369399 |
3 |
A locally active antiinflammatory macrolide (MLD987) for inhalation therapy of asthma. |
Novartis Institutes For Biomedical Research and Novartis Pharma Development |
22325943 |
71 |
Imidazo[1,2-a]pyrazines as novel PI3K inhibitors. |
Spanish National Cancer Research Centre (Cnio) |
22136433 |
67 |
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 |
78 |
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 |
17 |
Structure-based optimization of morpholino-triazines as PI3K and mTOR inhibitors. |
S*Bio |
22040023 |
63 |
Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1). |
Pfizer |
22177407 |
104 |
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 |
21981714 |
48 |
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 |
113 |
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 |
22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
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 |
54 |
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 |
21763134 |
57 |
Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors. |
Pfizer |
20561789 |
6 |
Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment. |
Sanofi-Aventis |
21636270 |
27 |
Structure-based design of thienobenzoxepin inhibitors of PI3-kinase. |
Genentech |
21621413 |
24 |
Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability. |
Dana-Farber Cancer Institute |
21495671 |
95 |
Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine. |
Genentech |
21438579 |
4 |
Isolation and structure of homotemsirolimuses A, B, and C. |
Wyeth Research |
21332118 |
157 |
Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors. |
Amgen |
21413798 |
174 |
Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents. |
Vertex Pharmaceuticals |
21388141 |
22 |
Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis. |
Korea Advanced Institute of Science and Technology |
21376583 |
232 |
Discovery of triazine-benzimidazoles as selective inhibitors of mTOR. |
Amgen |
21316229 |
12 |
Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. |
Chugai Pharmaceutical |
24900252 |
33 |
Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase Inhibitors |
TBA |
21269826 |
39 |
Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors. |
Pfizer |
21062009 |
70 |
Design, Synthesis, and Structure−Activity Relationships of 3-Ethynyl-1H-indazoles as Inhibitors of the Phosphatidylinositol 3-Kinase Signaling Pathway |
TBA |
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 |
20817449 |
19 |
4-methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors. |
Pfizer |
20797855 |
63 |
PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor. |
Pfizer |
20483602 |
23 |
5-ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-alpha and mTOR for the treatment of breast cancer. |
Wyeth Research |
20363128 |
42 |
Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors. |
Wyeth Research |
19894727 |
164 |
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 |
25 |
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 |
22 |
B-Raf kinase inhibitors: hit enrichment through scaffold hopping. |
Wyeth Research |
20303263 |
87 |
Novel benzofuran-3-one indole inhibitors of PI3 kinase-alpha and the mammalian target of rapamycin: hit to lead studies. |
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 |
19884006 |
47 |
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors. |
Wyeth Research |
20166671 |
85 |
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 |
19762236 |
9 |
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 |
52 |
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 |
25 |
Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR. |
Kudos Pharmaceuticals |
19916508 |
76 |
Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors. |
Wyeth Research |
19362830 |
47 |
Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors. |
Wyeth Research |
19317452 |
155 |
Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4. |
Wyeth Research |
18815050 |
34 |
4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors. |
Wyeth Research |
18644721 |
131 |
Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines. |
Ucb Pharma |
17562705 |
6 |
Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one. |
Stony Brook University |
16185865 |
4 |
Rapamycin analogs with reduced systemic exposure. |
Abbott Laboratories |
16143526 |
1 |
Novel indole alpha-methylene-gamma-lactones as potent inhibitors for AKT-mTOR signaling pathway kinases. |
Chinese Academy of Sciences |
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 |
32324396 |
17 |
p62/SQSTM1, a Central but Unexploited Target: Advances in Its Physiological/Pathogenic Functions and Small Molecular Modulators. |
China Pharmaceutical University |
32502336 |
79 |
Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models. |
Bayer |
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 |
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 |
27563401 |
8 |
CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model. |
Cellzome |
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 |
30629434 |
64 |
Discovery of Novel Dual Histone Deacetylase and Mammalian Target of Rapamycin Target Inhibitors as a Promising Strategy for Cancer Therapy. |
TBA |
31749911 |
68 |
Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors. |
Nestl� |
30582807 |
22 |
Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective. |
University Park Nottingham |
10411471 |
19 |
Evaluation of PMF scoring in docking weak ligands to the FK506 binding protein. |
Abbott Laboratories |
30975623 |
34 |
Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3K? selective inhibitors. |
Zydus Research Centre |
31693351 |
473 |
Discovery of 4 |
TBA |
31581005 |
29 |
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer. |
Ain Shams University |
31228810 |
162 |
Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
West China Hospital of Sichuan University |
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 |
32069401 |
27 |
Design, Synthesis, and Biological Evaluation of Imidazo[1,2- |
East China Normal University |
31082764 |
3 |
Design, synthesis and pharmacological evaluation of a novel mTOR-targeted anti-EV71 agent. |
National Engineering Research Center For The Emergency Drug |
31465220 |
139 |
A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor. |
University of Basel |
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 |
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 |
24345273 |
111 |
Design, synthesis, and biological activity of pyridopyrimidine scaffolds as novel PI3K/mTOR dual inhibitors. |
Universit£ |
24900667 |
3 |
Inhibition of mTOR Kinase and Cancer Treatment. |
Therachem Research Medilab (India) |
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 |
30015070 |
8 |
Synthesis and anticancer activity of new dihydropyrimidinone derivatives. |
Mansoura University |
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 |
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 |
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 |
29466002 |
193 |
Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening. |
University of Edinburgh |
29017786 |
35 |
Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
Spanish National Cancer Research Centre (Cnio) |
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 |
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 |
29107429 |
7 |
Discovery of 1-(3-aryl-4-chlorophenyl)-3-(p-aryl)urea derivatives against breast cancer by inhibiting PI3K/Akt/mTOR and Hedgehog signalings. |
Tsinghua University |
28947947 |
112 |
Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors. |
Novartis Institutes For Biomedical Research |
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 |
28409639 |
83 |
Design, Synthesis, and Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual Inhibitors. |
West China Hospital of Sichuan University |
28259529 |
31 |
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
The Ohio State University |
28526367 |
30 |
Discovery of a novel aminopyrazine series as selective PI3K? inhibitors. |
Astrazeneca |
29308895 |
24 |
Highly Selective, Potent, and Oral mTOR Inhibitor for Treatment of Cancer as Autophagy Inducer. |
Nankai University |
28571824 |
65 |
Design, synthesis and SAR of new-di-substituted pyridopyrimidines as ATP-competitive dual PI3K?/mTOR inhibitors. |
Temple University |
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 |
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 |
20030504 |
38 |
Fluorobenzoyl dipeptidyl derivatives as inhibitors of the Fasciola hepatica cysteine protease cathepsin L1. |
Dublin City University |
27595330 |
6 |
Small-molecule WNK inhibition regulates cardiovascular and renal function. |
Novartis Institutes |
12815170 |
15 |
[125I]A-312110, a novel high-affinity 1,4-dihydropyridine ATP-sensitive K+ channel opener: characterization and pharmacology of binding. |
Abbott Laboratories |
11907190 |
4 |
4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine hydrochloride (SSR125543A): a potent and selective corticotrophin-releasing factor(1) receptor antagonist. I. Biochemical and pharmacological characterization. |
Sanofi Synthelabo |
11882920 |
41 |
Characterization of phospholipase C activity at h5-HT2C compared with h5-HT2B receptors: influence of novel ligands upon membrane-bound levels of [3H]phosphatidylinositols. |
Institut De Recherches Servier |
11303063 |
11 |
Molecular and pharmacological characterization of muscarinic receptor subtypes in a rat parotid gland cell line: comparison with native parotid gland. |
Creighton University |
12616631 |
18 |
D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity. |
University of Queensland Brisbane |
19012568 |
7 |
Binding properties of the C-terminal domain of VIAF. |
The Burnham Institute For Medical Research |
16873019 |
6 |
MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells. |
Gpc Biotech |
18849971 |
56 |
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
University of California San Francisco |
18817367 |
28 |
Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. |
Abbott Laboratories |
17574423 |
44 |
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors. |
Pfizer |
17352464 |
51 |
Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors. |
Abbott Laboratories |
8879560 |
22 |
Structure-activity relationships of HIV-1 PR inhibitors containing AHPBA--II. Modification of pyrrolidine ring at P1' proline. |
Sankyo |
8893827 |
17 |
Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors. |
Upjohn |