PMID

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Article Title

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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

Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.

Merck

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

RhôNe-Poulenc Rorer

Class II Phosphoinositide 3-Kinases as Novel Drug Targets.

Curtin University

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

Infinity Pharmaceuticals

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

A Prospective Virtual Screening Study: Enriching Hit Rates and Designing Focus Libraries To Find Inhibitors of PI3Kd and PI3K¿.

Janssen Pharmaceutica

2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kd Selective Inhibitors.

Gilead Sciences

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

Identification of ETP-46321, a potent and orally bioavailable PI3Ka,d inhibitor.

Spanish National Cancer Research Centre (Cnio)

Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.

Amgen

Imidazo[1,2-a]pyrazines as novel PI3K inhibitors.

Spanish National Cancer Research Centre (Cnio)

Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability.

Dana-Farber Cancer Institute

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

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

Discovery of 6,7-dihydro-5H-pyrrolo[3,4-d] pyrimidine derivatives as a new class of ATR inhibitors.

Sichuan University

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

Spanish National Cancer Research Centre (Cnio)

Synthesis and biological evaluation of novel purinyl quinazolinone derivatives as PI3K?-specific inhibitors for the treatment of hematologic malignancies.

Sungkyunkwan University

Projected Dose Optimization of Amino- and Hydroxypyrrolidine Purine PI3K? Immunomodulators.

Merck

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

Glaxosmithkline R&D

Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.

Chinese Academy of Sciences

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

Structurally novel PI3K?/? dual inhibitors characterized by a seven-membered spirocyclic spacer: The SARs investigation and PK evaluation.

Anhui University of Chinese Medicine

Optimization of Versatile Oxindoles as Selective PI3K? Inhibitors.

Merck

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

Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.

Merck

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

University of Auckland

Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.

Merck And

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

Astrazeneca

Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3K?-selective inhibitors for treating B-cell-mediated malignancies.

Zhejiang University

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

The Exploration of Chirality for Improved Druggability within the Human Kinome.

University of Arkansas For Medical Sciences

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

Hutchison Medipharma

Evolution of PI3K? and ? Inhibitors for Inflammatory and Autoimmune Diseases.

Astrazeneca

Structure Overhaul Affords a Potent Purine PI3K? Inhibitor with Improved Tolerability.

TBA

Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.

Qingdao 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

Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.

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

Optimization and in vivo evaluation of pyrazolopyridines as a potent and selective PI3K? inhibitor.

Astellas Pharma

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

Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity.

Fudan University

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

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

Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168).

University of Michigan

Structure-Based Design of Tricyclic NF-?B Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K).

Genentech

Design, Synthesis, and Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual Inhibitors.

West China Hospital of Sichuan University

Design and synthesis of novel 6-aryl substituted 4-anilinequinazoline derivatives as potential PI3K? inhibitors.

Xi'An Jiaotong University

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

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£

Discovery of a Highly Selective STK16 Kinase Inhibitor.

Chinese Academy of Sciences

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