PMID

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Article Title

Organization

Discovery of triazole aminopyrazines as a highly potent and selective series of PI3Kd inhibitors.

Astrazeneca

Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety.

Xi'An Jiaotong University

Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors.

Hangzhou Xixi Hospital

Novel pyrazolo[1,5-a]pyridines with improved aqueous solubility as p110a-selective PI3 kinase inhibitors.

University of Auckland

Discovery of a Potent, Selective, and Orally Available PI3Kd Inhibitor for the Treatment of Inflammatory Diseases.

RhôNe-Poulenc Rorer

Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-¿ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.

Infinity Pharmaceuticals

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

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

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

Macrocyclization as a Source of Desired Polypharmacology. Discovery of Triple PI3K/mTOR/PIM Inhibitors.

Spanish National Cancer Research Centre (Cnio)

Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3K? with a Novel Binding Mode.

Glaxosmithkline R&D

Omipalisib inspired macrocycles as dual PI3K/mTOR inhibitors.

Spanish National Cancer Research Centre (Cnio)

Design, synthesis and biological activity of novel 2,3,4,5-tetra-substituted thiophene derivatives as PI3K? inhibitors with potent antitumor activity.

Guizhou Medical University

Discovery of Orally Efficacious Phosphoinositide 3-Kinase ? Inhibitors with Improved Metabolic Stability.

Gilead Sciences

Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of advanced solid tumors.

Chinese Academy of Sciences

Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3K? Inhibitors.

Amgen

Structure-Based Drug Design and Synthesis of PI3K?-Selective Inhibitor (PF-06843195).

Pfizer

Discovery of Potent and Selective PI3K? Inhibitors.

Arcus Biosciences

Discovery of an Atropisomeric PI3K? Selective Inhibitor through Optimization of the Hinge Binding Motif.

Gilead Sciences

Synthesis and biological evaluation of solubilized sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474.

University of Auckland

The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-

Astrazeneca

Discovery of 4

TBA

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

Design, Synthesis, and Biological Evaluation of Imidazo[1,2-

East China Normal University

Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3K?-PI3K? Dual Inhibitors.

Hutchison Medipharma

Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.

Qingdao University

Targeting the immunity protein kinases for immuno-oncology.

China Pharmaceutical University

Atropisomerism by Design: Discovery of a Selective and Stable Phosphoinositide 3-Kinase (PI3K) ? Inhibitor.

Gilead Sciences

Optimization of Orally Bioavailable PI3K? Inhibitors and Identification of Vps34 as a Key Selectivity Target.

Glaxosmithkline

Discovery of 4-Methylquinazoline Based PI3K Inhibitors for the Potential Treatment of Idiopathic Pulmonary Fibrosis.

TBA

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

Piperidinyl-embeded chalcones possessing anti PI3K? inhibitory properties exhibit anti-atopic properties in preclinical models.

Inserm 1052/Cnrs 5286/University of Lyon

Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR.

Wuxi Apptec (Shanghai) Co.

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

Discovery and biological evaluation of novel pyrazolopyridine derivatives as potent and orally available PI3K? inhibitors.

Astellas Pharma

Novel 4-aminoquinazoline derivatives induce growth inhibition, cell cycle arrest and apoptosis via PI3K? inhibition.

Shenyang Pharmaceutical University

Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines.

Shanghai Haiyan Pharmaceutical Technology

Identification of novel PI3K inhibitors through a scaffold hopping strategy.

Spanish National Cancer Research Centre (Cnio)

Synthesis and biological evaluation of sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474.

University of Auckland

Discovery of a Novel Inhaled PI3K? Inhibitor for the Treatment of Respiratory Diseases.

TBA

Designing multi-targeted agents: An emerging anticancer drug discovery paradigm.

Hunan University of Chinese Medicine

Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-? Inhibitors.

Pharmaron-Beijing

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)

Design and Synthesis of Soluble and Cell-Permeable PI3K? Inhibitors for Long-Acting Inhaled Administration.

Astrazeneca

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

Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury.

Targegen

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