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 |
28017532 |
140 |
Discovery of triazole aminopyrazines as a highly potent and selective series of PI3Kd inhibitors. |
Astrazeneca |
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 |
27923617 |
70 |
Novel pyrazolo[1,5-a]pyridines with improved aqueous solubility as p110a-selective PI3 kinase inhibitors. |
University of Auckland |
27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
28105286 |
65 |
Discovery of a Potent, Selective, and Orally Available PI3Kd Inhibitor for the Treatment of Inflammatory Diseases. |
RhôNe-Poulenc Rorer |
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 |
27644332 |
59 |
Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
Curtin University |
27660692 |
70 |
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-¿ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate. |
Infinity Pharmaceuticals |
27186676 |
186 |
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
West China Hospital of Sichuan University |
27043133 |
16 |
A Prospective Virtual Screening Study: Enriching Hit Rates and Designing Focus Libraries To Find Inhibitors of PI3Kd and PI3K¿. |
Janssen Pharmaceutica |
27189888 |
11 |
Optimization of the phenylurea moiety in a phosphoinositide 3-kinase (PI3K) inhibitor to improve water solubility and the PK profile by introducing a solubilizing group and ortho substituents. |
Chugai Pharmaceutical |
26980109 |
42 |
2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kd Selective Inhibitors. |
Gilead Sciences |
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 |
23644197 |
51 |
Synthesis and biological evaluation of novel phosphatidylinositol 3-kinase inhibitors: Solubilized 4-substituted benzimidazole analogs of 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474). |
University of Auckland |
23291120 |
2 |
Synthesis and biological evaluation of novel coumarin-pyrazoline hybrids endowed with phenylsulfonyl moiety as antitumor agents. |
Cairo University |
22520259 |
65 |
Identification of ETP-46321, a potent and orally bioavailable PI3Ka,d inhibitor. |
Spanish National Cancer Research Centre (Cnio) |
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 |
23040731 |
4 |
Viridin analogs derived from steroidal building blocks. |
University of Connecticut |
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£ |
18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
22325943 |
71 |
Imidazo[1,2-a]pyrazines as novel PI3K inhibitors. |
Spanish National Cancer Research Centre (Cnio) |
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 |
21322566 |
61 |
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 |
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 |
17562705 |
6 |
Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one. |
Stony Brook University |
16464575 |
7 |
Synthesis of fluorescent derivatives of wortmannin and demethoxyviridin as probes for phosphatidylinositol 3-kinase. |
State University of New York-Esf |
32317209 |
8 |
Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives. |
Central South University |
32551006 |
134 |
Discovery of an Atropisomeric PI3K? Selective Inhibitor through Optimization of the Hinge Binding Motif. |
Gilead Sciences |
11206452 |
14 |
3-Deoxy-3-substituted-D-myo-inositol imidazolyl ether lipid phosphates and carbonate as inhibitors of the phosphatidylinositol 3-kinase pathway and cancer cell growth. |
Georgetown University Medical Center |
31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
30850264 |
108 |
Synthesis and biological evaluation of solubilized sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474. |
University of Auckland |
27491711 |
422 |
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties. |
Merck And |
31851518 |
61 |
The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5- |
Astrazeneca |
30878826 |
45 |
Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3K?-selective inhibitors for treating B-cell-mediated malignancies. |
Zhejiang University |
31693351 |
473 |
Discovery of 4 |
TBA |
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 |
32069401 |
27 |
Design, Synthesis, and Biological Evaluation of Imidazo[1,2- |
East China Normal University |
31550151 |
17 |
The Exploration of Chirality for Improved Druggability within the Human Kinome. |
University of Arkansas For Medical Sciences |
31074988 |
95 |
Rational Design of 5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine (VX-970, M6620): Optimization of Intra- and Intermolecular Polar Interactions of a New Ataxia Telangiectasia Mutated and Rad3-Related (ATR) Kinase Inhibitor. |
Vertex Pharmaceuticals (Europe) |
31033293 |
77 |
Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3K?-PI3K? Dual Inhibitors. |
Hutchison Medipharma |
30582813 |
67 |
Evolution of PI3K? and ? Inhibitors for Inflammatory and Autoimmune Diseases. |
Astrazeneca |
30986068 |
112 |
Structure Overhaul Affords a Potent Purine PI3K? Inhibitor with Improved Tolerability. |
TBA |
30418766 |
35 |
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
Qingdao University |
30530193 |
64 |
Targeting the immunity protein kinases for immuno-oncology. |
China Pharmaceutical University |
30015489 |
16 |
Atropisomerism by Design: Discovery of a Selective and Stable Phosphoinositide 3-Kinase (PI3K) ? Inhibitor. |
Gilead Sciences |
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 |
31335136 |
29 |
Discovery of 4-Methylquinazoline Based PI3K Inhibitors for the Potential Treatment of Idiopathic Pulmonary Fibrosis. |
TBA |
31117517 |
103 |
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases. |
TBA |
28106991 |
136 |
Discovery of a Phosphoinositide 3-Kinase (PI3K) ?/? Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3K? Potency in a PI3K?-Selective Template by Targeting Nonconserved Asp856. |
Gilead Sciences |
30071408 |
56 |
Difuran-substituted quinoxalines as a novel class of PI3K? H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship. |
Chongqing University |
29046238 |
17 |
1,3,5-Triazines: A promising scaffold for anticancer drugs development. |
Universit£ |
30237123 |
12 |
Piperidinyl-embeded chalcones possessing anti PI3K? inhibitory properties exhibit anti-atopic properties in preclinical models. |
Inserm 1052/Cnrs 5286/University of Lyon |
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 |
29907471 |
25 |
Optimization and in vivo evaluation of pyrazolopyridines as a potent and selective PI3K? inhibitor. |
Astellas Pharma |
29631787 |
21 |
Discovery and biological evaluation of novel pyrazolopyridine derivatives as potent and orally available PI3K? inhibitors. |
Astellas Pharma |
29475582 |
8 |
Novel 4-aminoquinazoline derivatives induce growth inhibition, cell cycle arrest and apoptosis via PI3K? inhibition. |
Shenyang Pharmaceutical University |
30034607 |
60 |
Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines. |
Shanghai Haiyan Pharmaceutical Technology |
28835805 |
45 |
Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. |
Fudan University |
28800461 |
16 |
Design, synthesis, and biological evaluation of novel 3-substituted imidazo[1,2-a]pyridine and quinazolin-4(3H)-one derivatives as PI3K? inhibitors. |
Shenyang Pharmaceutical University |
29017786 |
35 |
Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
Spanish National Cancer Research Centre (Cnio) |
28958845 |
147 |
Synthesis and biological evaluation of sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474. |
University of Auckland |
30351000 |
119 |
Discovery of a Novel Inhaled PI3K? Inhibitor for the Treatment of Respiratory Diseases. |
TBA |
28494256 |
11 |
Designing multi-targeted agents: An emerging anticancer drug discovery paradigm. |
Hunan University of Chinese Medicine |
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 |
28005357 |
59 |
Structure-Based Design of Tricyclic NF-?B Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K). |
Genentech |
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 |
28325601 |
3 |
Design and synthesis of novel 6-aryl substituted 4-anilinequinazoline derivatives as potential PI3K? inhibitors. |
Xi'An Jiaotong 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 |
28404374 |
81 |
Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
Spanish National Cancer Research Centre (Cnio) |
28520415 |
91 |
Design and Synthesis of Soluble and Cell-Permeable PI3K? Inhibitors for Long-Acting Inhaled Administration. |
Astrazeneca |
28489362 |
12 |
Atropisomerism and Conformational Equilibria: Impact on PI3K? Inhibition of 2-((6-Amino-9H-purin-9-yl)methyl)-5-methyl-3-(o-tolyl)quinazolin-4(3H)-one (IC87114) and Its Conformationally Restricted Analogs. |
Universit£ |
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 |
27082499 |
10 |
Discovery of a Highly Selective STK16 Kinase Inhibitor. |
Chinese Academy of Sciences |
9405385 |
26 |
Cloning and expressional characterization of a novel galanin receptor. Identification of different pharmacophores within galanin for the three galanin receptor subtypes. |
Schering-Plough Research Institute |
19848404 |
44 |
Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase. |
Wyeth Research |
19645448 |
48 |
ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin: Design and Synthesis of Highly Potent and Selective Pyrazolopyrimidines |
Wyeth Research |
19209891 |
34 |
New Insights into the Design of Inhibitors of Human S-Adenosylmethionine Decarboxylase: Studies of Adenine C(8) Substitution in Structural Analogues of S-Adenosylmethionine (dagger). |
Cornell University |
19228017 |
52 |
Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold. |
Genentech |
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 |
17685602 |
33 |
Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction. |
Targegen |
17172449 |
20 |
Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury. |
Targegen |
18754654 |
19 |
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
Piramed Pharma |
14722321 |
9 |
A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. |
Johnson & Johnson Pharmaceutical |
18269228 |
93 |
Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy. |
Wyeth Research |
11520201 |
10 |
X-Ray crystal structures of Candida albicans dihydrofolate reductase: high resolution ternary complexes in which the dihydronicotinamide moiety of NADPH is displaced by an inhibitor. |
Gsk |
17574423 |
44 |
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors. |
Pfizer |
11090628 |
5 |
Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine. |
Mrc |
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 |