PMID

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Article Title

Organization

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

Astrazeneca

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

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

Hangzhou Xixi Hospital

Non-kinase targets of protein kinase inhibitors.

The University of Sydney

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

6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors.

Csir-Indian Institute of Integrative Medicine

Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties.

Novartis Institutes For Biomedical Research

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

Discovery and antiplatelet activity of a selective PI3Kß inhibitor (MIPS-9922).

Monash University

Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3Kd.

TBA

Imidazopyridazine Inhibitors of PI3Kß.

Dart Neuroscience

Synthesis of linear and angular aryl-morpholino-naphth-oxazines, their DNA-PK, PI3K, PDE3A and antiplatelet activity.

La Trobe University

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

Class II Phosphoinositide 3-Kinases as Novel Drug Targets.

Curtin University

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

Discovery of a Series of 5,11-Dihydro-6

Dana-Farber Cancer Institute

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

Infinity Pharmaceuticals

Discovery of novel 7-azaindoles as PDK1 inhibitors.

Merck

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

Gilead Sciences

Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIß.

University of California

Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.

Novartis Institutes For Biomedical Research

Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo.

Novartis Institutes For Biomedical Research

Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.

Saarland University

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

Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines.

La Trobe University

Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma.

Second Military Medical University

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

Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.

Shandong University

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

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

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

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

Discovery of potent, selective small molecule inhibitors ofa-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIa).

Astrazeneca

Design, synthesis and biological evaluation of novel condensed pyrrolo[1,2-c]pyrimidines featuring morpholine moiety as PI3Ka inhibitors.

Cairo University

Design of selective PI3Ka inhibitors starting from a promiscuous pan kinase scaffold.

Astrazeneca

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

Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿.

Vertex Pharmaceuticals

Discovery of a Potent Class of PI3Ka Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).

Glaxosmithkline

Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors.

Pkucare Pharmaceutical R & D Center

Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2.

Astrazeneca

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

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

6,7-Dihydrobenzo[f]benzo[4,5]imidazo[1,2-d][1,4]oxazepine derivatives as selective inhibitors of PI3Ka.

Nanjing University

Synthesis and SAR study of potent and selective PI3Kd inhibitors.

Amgen

Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.

University Hospital Hradec Kralove

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

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

Quinalozinones as Inhibitors of Class I PI3K Kinases.

Dart Neuroscience

Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.

Monash University (Parkville Campus)

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

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

Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).

Icahn School of Medicine At Mount Sinai

Discovery and optimization of pyrimidone indoline amide PI3Kß inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.

Sanofi

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

Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K.

Novartis Institutes For Biomedical Research

A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors.

Genentech

Identification of GNE-293, a potent and selective PI3Kd inhibitor: navigating in vitro genotoxicity while improving potency and selectivity.

Genentech

Design, synthesis and biological evaluation of novel aminothiazoles as antiviral compounds acting against human rhinovirus.

Boehringer Ingelheim (Canada)

Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.

Novartis Institutes For Biomedical Research

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

Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinaseß isoform.

Genentech

Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).

Exelixis

Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.

Astrazeneca

Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design.

Pfizer

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

Regioselective synthesis of 5- and 6-methoxybenzimidazole-1,3,5-triazines as inhibitors of phosphoinositide 3-kinase.

Monash Institute of Pharmaceutical Sciences

L-Aminoacyl-triazine derivatives are isoform-selective PI3K? inhibitors that target non-conserved Asp862 of PI3K?

Monash University (Parkville Campus)

Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Ka.

Celgene Avilomics Research

Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors.

TBA

PI3Kd and PI3K¿ as targets for autoimmune and inflammatory diseases.

Amgen

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

Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold.

Amgen

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

Recent results in protein kinase inhibition for tropical diseases.

Montclair State University

Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.

Genentech

Discovery and in vivo evaluation of dual PI3Kß/d inhibitors.

Amgen

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

Discovery of novel PI3-kinased specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.

Genentech

Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.

Amgen

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

Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.

Exelixis

Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3Kß inhibitors.

Sanofi

Potent and selective inhibitors of PI3Kd: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.

Genentech

Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway.

Novartis Institutes For Biomedical Research

SAR studies around a series of triazolopyridines as potent and selective PI3K¿ inhibitors.

Cellzome

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

Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.

Spanish National Cancer Research Centre (Cnio)

Discovery of novel PI3K¿/d inhibitors as potential agents for inflammation.

Cellzome

Synthesis, biological evaluation and molecular docking studies of 1,3,4-oxadiazole derivatives as potential immunosuppressive agents.

Nanjing University

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

Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.

TBA

Features of selective kinase inhibitors.

University of California San Francisco

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

Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.

Novartis Institute For Biomedical Research

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

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

Rational design of phosphoinositide 3-kinasea inhibitors that exhibit selectivity over the phosphoinositide 3-kinaseß isoform.

Genentech

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

Novel pyrazolo[1,5-a]pyridines as p110a-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR.

University of Auckland

Discovery of pyrazolo[1,5-a]pyridines as p110a-selective PI3 kinase inhibitors.

University of Auckland

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

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

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

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

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

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

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.

Genentech

Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.

Amgen

Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.

Amgen

Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799.

Chugai Pharmaceutical

Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase Inhibitors

TBA

Discovery of novel class 1 phosphatidylinositide 3-kinases (PI3K) fragment inhibitors through structure-based virtual screening.

Astrazeneca R & D M£Lndal

Design, Synthesis, and Structure−Activity Relationships of 3-Ethynyl-1H-indazoles as Inhibitors of the Phosphatidylinositol 3-Kinase Signaling Pathway

TBA

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

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.

Genentech

PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.

Pfizer

AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Ambit Biosciences

The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.

Medical Research Council-Laboratory of Molecular Biology

5-ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-alpha and mTOR for the treatment of breast cancer.

Wyeth Research

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

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.

Genentech

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

The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase.

Kudos Pharmaceuticals

Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.

Wyeth Research

Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: discovery of highly potent and selective analogs with improved human microsomal stability.

Wyeth Research

Phosphoinositide-3-kinase (PI3K) inhibitors: identification of new scaffolds using virtual screening.

University of Auckland

Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors.

Wyeth Research

Optimization of a series of multi-isoform PI3 kinase inhibitors.

Ucb Pharma

Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines.

Ucb Pharma

4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase.

Ucb Pharma

Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors.

University of Auckland

Discovery of 4-oxo-4,5-dihydropyrazolo[1,5-a]quinoxaline-7-carboxamide derivatives as PI3K? inhibitors via virtual screening and docking-based structure optimization.

Zhejiang University

Design, synthesis and bioactivity evaluation of a series of quinazolinone derivatives as potent PI3K? antagonist.

Southern Medical University

Dual Kinase-Bromodomain Inhibitors in Anticancer Drug Discovery: A Structural and Pharmacological Perspective.

University of Modena and Reggio Emilia

Design strategies, structure activity relationship and mechanistic insights for purines as kinase inhibitors.

Guru Nanak Dev University

Developing a Naïve Bayesian Classification Model with PI3K? structural features for virtual screening against PI3K?: Combining molecular docking and pharmacophore based on multiple PI3K? conformations.

Jiangnan University

Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors.

Astrazeneca

Design, synthesis and in vitro biological evaluation of 2-aminopyridine derivatives as novel PI3K? inhibitors for hematological cancer.

Fudan University

4-Aminopyrazolopyrimidine scaffold and its deformation in the design of tyrosine and serine/threonine kinase inhibitors in medicinal chemistry.

Yangtze University

Imidazo[1,2-b]pyridazine as privileged scaffold in medicinal chemistry: An extensive review.

Universite de Tours

4-(3H)-quinazolinones N-3 substituted with a five membered heterocycle: A promising scaffold towards bioactive molecules.

Chimiche E Farmaceutiche - Sezione Di Chimica E Tecnologie Farmaceutiche - Universit£

Research progress of mTOR inhibitors.

Jilin University

Molecular hybrids: A five-year survey on structures of multiple targeted hybrids of protein kinase inhibitors for cancer therapy.

Al-Azhar University

Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions.

Sichuan University

Targeting the PI3K/AKT/mTOR Signaling Pathway in the Treatment of Human Diseases: Current Status, Trends, and Solutions.

South China University of Technology

Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3K?-selective template.

Anhui University of Chinese Medicine

Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.

Serono Pharmaceutical Research Institute

Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021).

University of Hradec Kralove

Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.

Menoufia University

Design and Optimization of Thienopyrimidine Derivatives as Potent and Selective PI3K? Inhibitors for the Treatment of B-Cell Malignancies.

Chinese Academy of Medical Sciences and Peking Union Medical College

Discovery of Novel Indazoles as Potent and Selective PI3K? Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma.

Zhejiang University

Design, Synthesis, and Structure-Activity Relationship Optimization of Pyrazolopyrimidine Amide Inhibitors of Phosphoinositide 3-Kinase ? (PI3K?).

Arcus Biosciences

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3K?.

Genentech

Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies.

Tianjin University

Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases.

National Clinical Research Center For Geriatrics

FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.

Zhengzhou University

Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.

Hefei University of Technology

Discovery of Novel Phosphoinositide-3-Kinase ? Inhibitors with High Selectivity, Excellent Bioavailability, and Long-Acting Efficacy for Gastric Cancer.

China Pharmaceutical University

Identification and optimization of a novel series of selective PIP5K inhibitors.

Astrazeneca

Optimization of hERG and Pharmacokinetic Properties for Basic Dihydro-8

Astrazeneca

Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.

Novartis Institutes For Biomedical Research

Kinase Inhibitors as Underexplored Antiviral Agents.

Centro De Investigaciones Biol�Gicas Margarita Salas (Csic)

Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.

Csir-Indian Institute of Integrative Medicine

Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review.

Bioland Laboratory (Guangzhou Regenerative Medicine and Health - Guangdong Laboratory)

Discovery, Optimization, and Evaluation of Potent and Selective PI3K?-? Dual Inhibitors for the Treatment of B-cell Malignancies.

West China Hospital

Discovery of novel 7,8-dihydropteridine-6(5H)-one-based DNA-PK inhibitors as potential anticancer agents via scaffold hopping strategy.

Zhuhai Campus of Zunyi Medical University

Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.

Chinese Academy of Medical Sciences & Peking Union Medical College

Discovery of 2-Methyl-2-(4-(2-methyl-8-(1

West China Hospital of Sichuan University

Phenotypic Discovery of Triazolo[1,5-

Technical University Dortmund

Design, Synthesis, Biological Evaluation, and Computational Studies of Novel Fluorinated Candidates as PI3K Inhibitors: Targeting Fluorophilic Binding Sites.

Huazhong Agricultural University

Synthesis and bioevaluation of diaryl urea derivatives as potential antitumor agents for the treatment of human colorectal cancer.

Guizhou Medical University

Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors.

The University of Michigan Medical School

Design, Synthesis, and Biological Evaluation of a Novel Photocaged PI3K Inhibitor toward Precise Cancer Treatment.

TBA

Discovery of AZD8154, a Dual PI3K?? Inhibitor for the Treatment of Asthma.

Astrazeneca

Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3K? inhibitor: Design, synthesis and biological evaluation.

Fudan University

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

Merck

Discovery and Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase ?.

Novartis Institutes For Biomedical Research

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

Glaxosmithkline R&D

Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity.

Fudan University

Discovery of a new series of PI3K-? inhibitors from Virtual Screening.

Merck

Pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors.

Guangzhou Institutes of Biomedicine and Health

Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment.

Southern Medical University

Discovery of novel and potent PARP/PI3K dual inhibitors for the treatment of cancer.

China Pharmaceutical University

Synthetic Lethality through the Lens of Medicinal Chemistry.

Istituto Italiano Di Tecnologia

Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors.

Guizhou Medical University

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

Gilead Sciences

Structural optimization towards promising ?-methyl-4-acrylamido quinoline derivatives as PI3K/mTOR dual inhibitors for anti-cancer therapy: The in vitro and in vivo biological evaluation.

Jiaxing University

Discovery of novel PARP/PI3K dual inhibitors with high efficiency against BRCA-proficient triple negative breast cancer.

China Pharmaceutical University

Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3K? inhibitors.

Southwest Jiaotong University

Discovery of a Potent and Selective PI3K? Inhibitor (

Lupin

Discovery of 2-(5-(quinolin-6-yl)-1,3,4-oxadiazol-2-yl)acetamide derivatives as novel PI3K? inhibitors via docking-based virtual screening.

Zhejiang University

4-(Difluoromethyl)-5-(4-((3

University of Basel

Research advances on selective phosphatidylinositol 3 kinase ? (PI3K?) inhibitors.

Xi'An Jiaotong University

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 novel quinazoline derivatives as potent PI3K? inhibitors with high selectivity.

China Pharmaceutical University

Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.

A*Star

Discovery of (

Hefei Institutes of Physical Science

Discovery of novel 1,3,5-triazine derivatives as potent inhibitor of cervical cancer via dual inhibition of PI3K/mTOR.

Maternal and Child Health Hospital of Hubei Province

Discovery of 6'-chloro-N-methyl-5'-(phenylsulfonamido)-[3,3'-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium.

Chinese Academy of Sciences

Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors.

Chinese Academy of Medical Sciences and Peking Union Medical College

Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-

University of Edinburgh

Optimization of Versatile Oxindoles as Selective PI3K? Inhibitors.

Merck

Design, synthesis, and biological evaluation of some novel 4-aminoquinazolines as Pan-PI3K inhibitors.

Shenyang Pharmaceutical University

Discovery of 3-Quinazolin-4(3

Luoxin Pharmaceutical (Shanghai) Co.

Design and Development of a Macrocyclic Series Targeting Phosphoinositide 3-Kinase ?.

Gsk Medicines Research Centre

Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives.

Central South University

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

Merck

Synthesis and antitumor activity evaluation of 4,6-disubstituted quinazoline derivatives as novel PI3K inhibitors.

Xi'An Jiaotong University

Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.

Glaxosmithkline R&D

Development of single and mixed isoform selectivity PI3K? inhibitors by targeting Asn836 of PI3K?.

Monash University

Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.

Novartis Institutes For Biomedical Research

Discovery and SAR of pyrrolo[2,1-f][1,2,4]triazin-4-amines as potent and selective PI3K? inhibitors.

Bristol-Myers Squibb

Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3K?.

China Pharmaceutical University

Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of

University of Nottingham

INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3K?).

Incyte

Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.

National Center For Advancing Translational Sciences

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

Astrazeneca

Synthesis and biological evaluation of 4-(piperid-3-yl)amino substituted 6-pyridylquinazolines as potent PI3K? inhibitors.

Xi'An Jiaotong University

Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective.

University Park Nottingham

Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3K? selective inhibitors.

Zydus Research Centre

Design of selective PI3K? inhibitors using an iterative scaffold-hopping workflow.

Merck

Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach.

Glaxosmithkline R&D

Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders.

Novartis Institutes For Biomedical Research

Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy.

TBA

Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.

Ain Shams University

Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents.

Chengdu University

Optimization of 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidines to generate a highly selective PI3K? inhibitor.

Astellas Pharma

Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3K?.

School of Traditional Chinese Pharmacy

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

Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.

Eberhard Karls University T£Bingen

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

TBA

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

Targeting the immunity protein kinases for immuno-oncology.

China Pharmaceutical University

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

Glaxosmithkline

A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor.

University of Basel

Why Some Targets Benefit from beyond Rule of Five Drugs.

Boston University

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

Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.

China Pharmaceutical University

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

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

Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation.

Zhejiang University

Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.

Novartis Institutes For Biomedical Research

Design, synthesis, and biological activity of pyridopyrimidine scaffolds as novel PI3K/mTOR dual inhibitors.

Universit£

[3a,4]-Dihydropyrazolo[1,5a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase ? Inhibitors.

Glaxosmithkline

Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors.

Xi'An Jiaotong University

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

Difuran-substituted quinoxalines as a novel class of PI3K? H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship.

Chongqing University

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

Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3K? H1047R mutant inhibitors.

Chongqing University

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

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

Discovery of novel quinazolinone derivatives as high potent and selective PI3K? and PI3K?/? inhibitors.

Shandong University

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

Astellas Pharma

Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.

Astrazeneca

Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3K?) inhibitors.

Xi'An Jiaotong University

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)

Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors.

Chinese Academy of Medical Sciences and Peking Union Medical College

Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.

Astrazeneca

Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3K?.

Shenyang Pharmaceutical University

Discovery of pyrazolopyrimidine derivatives as novel inhibitors of ataxia telangiectasia and rad3 related protein (ATR).

Integral Biosciences

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

TBA

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

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

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

From PIM1 to PI3K? via GSK3?: Target Hopping through the Kinome.

Glaxosmithkline

Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.

Novartis Institutes For Biomedical Research

Design of Selective Benzoxazepin PI3K? Inhibitors Through Control of Dihedral Angles.

Genentech

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

Potential of PI3K? Inhibitors in the Treatment of Cancer and Other Diseases.

Therachem Research Medilab (India)

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

Synthesis and biological evaluation of 8-aryl-2-morpholino-7-O-substituted benzo[e][1,3]oxazin-4-ones against DNA-PK, PI3K, PDE3A enzymes and platelet aggregation.

La Trobe University

SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3K?) inhibitors.

Shanghai Institute of Materia Medica (Simm)

Discovery of a novel aminopyrazine series as selective PI3K? inhibitors.

Astrazeneca

Identification of highly potent and selective PI3K? inhibitors.

Bristol-Myers Squibb

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

Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase? (PI3K?) Inhibitor for the Treatment of Immunological Disorders.

Bristol-Myers Squibb

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 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

Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases.

Spanish National Cancer Research Center (Cnio)

Discovery of dual inhibitors of the immune cell PI3Ks p110delta and p110gamma: a prototype for new anti-inflammatory drugs.

University of California San Francisco

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.

University of California San Francisco