PMID

Data

Article Title

Organization

Design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine derivatives as mTOR inhibitors.

Peking University

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

Non-kinase targets of protein kinase inhibitors.

The University of Sydney

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

Csir-Indian Institute of Integrative Medicine

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

Imidazopyridazine Inhibitors of PI3Kß.

Dart Neuroscience

Class II Phosphoinositide 3-Kinases as Novel Drug Targets.

Curtin University

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

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

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.

Genentech

Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.

Zhejiang University

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

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

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

Second Military Medical University

Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.

Hanyang University

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

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

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

4-(N-Phenyl-N'-substituted benzenesulfonyl)-6-(4-hydroxyphenyl)quinolines as inhibitors of mammalian target of rapamycin.

India Academy of Scientific & Innovative Research (Acsir)

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

Astrazeneca

Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115.

Celgene

Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.

Celgene

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

Pkucare Pharmaceutical R & D Center

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

Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Ka inhibitors.

Jiangxi Science & Technology Normal University

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

Astrazeneca

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

University Hospital Hradec Kralove

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

Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents.

Shenyang Pharmaceutical University

Development of synthetic lethality anticancer therapeutics.

The University of Texas M.D. Anderson Cancer Center

Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors.

Novartis Institutes For Biomedical Research

Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors.

Novartis Institutes For Biomedical Research

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

Monash University (Parkville Campus)

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

Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511.

Amgen

Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents.

Shenyang Pharmaceutical University

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

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

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

Virtual screening and biochemical evaluation to identify new inhibitors of mammalian target of rapamycin (mTOR).

Sejong University

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

Sanofi

Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach.

Merck Research Laboratories

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

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

Genentech

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

Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series.

Pfizer

Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.

Celgene

Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).

Genentech

Selective 3-phosphoinositide-dependent kinase 1 (PDK1) inhibitors: dissecting the function and pharmacology of PDK1.

Glaxosmithkline

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

Astrazeneca

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

Genentech

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

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

Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands.

Glaxo Wellcome

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

Spanish National Cancer Research Centre (Cnio)

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

Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.

Genentech

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinasea.

Genentech

Recent results in protein kinase inhibition for tropical diseases.

Montclair State University

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

Amgen

Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.

Amgen

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

Amgen

Identification of pyrimidine derivatives as hSMG-1 inhibitors.

Pfizer

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

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

Novartis Institutes For Biomedical Research

Conformationally-restricted cyclic sulfones as potent and selective mTOR kinase inhibitors.

Pfizer

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)

Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Ka and mTOR.

Pfizer

Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor.

Astrazeneca

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

Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity.

TBA

Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.

Hanyang University

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

The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain.

Stanford University

Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.

The Scripps Research Institute

A locally active antiinflammatory macrolide (MLD987) for inhalation therapy of asthma.

Novartis Institutes For Biomedical Research and Novartis Pharma Development

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

Spanish National Cancer Research Centre (Cnio)

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

Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2-ones as potent and selective mTOR kinase inhibitors.

Celgene

Structure-based optimization of morpholino-triazines as PI3K and mTOR inhibitors.

S*Bio

Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).

Pfizer

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

Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.

Hanyang University

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

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

Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.

Pfizer

Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment.

Sanofi-Aventis

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

Genentech

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

Dana-Farber Cancer Institute

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

Genentech

Isolation and structure of homotemsirolimuses A, B, and C.

Wyeth Research

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

Amgen

Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents.

Vertex Pharmaceuticals

Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis.

Korea Advanced Institute of Science and Technology

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

Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors.

Pfizer

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

TBA

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

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

Genentech

4-methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors.

Pfizer

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

Pfizer

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

Wyeth Research

Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.

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

Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors.

Wyeth Research

B-Raf kinase inhibitors: hit enrichment through scaffold hopping.

Wyeth Research

Novel benzofuran-3-one indole inhibitors of PI3 kinase-alpha and the mammalian target of rapamycin: hit to lead studies.

Wyeth Research

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

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

4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).

Wyeth Research

Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.

Wyeth Research

Selectively nonselective kinase inhibition: striking the right balance.

Schering-Plough

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

Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 1-substituent.

Wyeth Research

Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies.

Wyeth Research

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

Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.

Wyeth Research

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

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

Wyeth Research

Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR.

Kudos Pharmaceuticals

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

Wyeth Research

Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.

Wyeth Research

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

4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.

Wyeth Research

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

Ucb Pharma

Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one.

Stony Brook University

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

University of Hradec Kralove

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

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

Hefei University of Technology

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

Sichuan University

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

Novartis Institutes For Biomedical Research

Rapamycin analogs with reduced systemic exposure.

Abbott Laboratories

Novel indole alpha-methylene-gamma-lactones as potent inhibitors for AKT-mTOR signaling pathway kinases.

Chinese Academy of Sciences

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

Csir-Indian Institute of Integrative Medicine

Recent advances in DDR (DNA damage response) inhibitors for cancer therapy.

Hubei Polytechnic University

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

West China Hospital of Sichuan University

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

Recent advances in development of hetero-bivalent kinase inhibitors.

Cha University

Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.

University of Newcastle

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

Guizhou Medical University

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

Spanish National Cancer Research Centre (Cnio)

Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.

South China University of Technology

BAY-8400: A Novel Potent and Selective DNA-PK Inhibitor which Shows Synergistic Efficacy in Combination with Targeted Alpha Therapies.

Bayer

Structure-Based Exploration of Selectivity for ATM Inhibitors in Huntington's Disease.

Charles River

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

Chinese Academy of Sciences

Identification and optimization of 3-bromo-N'-(4-hydroxybenzylidene)-4-methylbenzohydrazide derivatives as mTOR inhibitors that induce autophagic cell death and apoptosis in triple-negative breast cancer.

Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre

Omipalisib inspired macrocycles as dual PI3K/mTOR inhibitors.

Spanish National Cancer Research Centre (Cnio)

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

China Pharmaceutical University

Ring closure strategy leads to potent RIPK3 inhibitors.

Soochow University

Design, synthesis and biological evaluation of dual mTOR/HDAC6 inhibitors in MDA-MB-231 cells.

Harbin Medical University

Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy.

Anhui University of Chinese Medicine

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

Guizhou Medical University

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

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

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

Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood-brain barrier permeability.

University of Basel

Discovery and SAR of Novel Disubstituted Quinazolines as Dual PI3Kalpha/mTOR Inhibitors Targeting Breast Cancer.

Temple University

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

University of Basel

Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis.

Sichuan University and Collaborative Innovation Center

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

Pfizer

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

A*Star

Discovery and Development of SPR519 as a Potent, Selective, and Orally Bioavailable Inhibitor of PI3K? and mTOR Kinases for the Treatment of Solid Tumors.

Sphaera Pharma

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

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

University of Edinburgh

Preclinical Development of PQR514, a Highly Potent PI3K Inhibitor Bearing a Difluoromethyl-Pyrimidine Moiety.

University of Basel

p62/SQSTM1, a Central but Unexploited Target: Advances in Its Physiological/Pathogenic Functions and Small Molecular Modulators.

China Pharmaceutical University

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

Pyrazolopyrimide library screening in glioma cells discovers highly potent antiproliferative leads that target the PI3K/mTOR pathway.

University of Edinburgh

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

Merck

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

Glaxosmithkline R&D

Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.

Astrazeneca

CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model.

Cellzome

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

Novartis Institutes For Biomedical Research

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

China Pharmaceutical University

Discovery of Novel Dual Histone Deacetylase and Mammalian Target of Rapamycin Target Inhibitors as a Promising Strategy for Cancer Therapy.

TBA

Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors.

Nestl�

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

University Park Nottingham

Evaluation of PMF scoring in docking weak ligands to the FK506 binding protein.

Abbott Laboratories

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

Zydus Research Centre

Discovery of 4

TBA

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

Ain Shams 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

Rational discovery of a highly novel and selective mTOR inhibitor.

Takeda California

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

School of Traditional Chinese Pharmacy

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University of Basel

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

East China Normal University

Design, synthesis and pharmacological evaluation of a novel mTOR-targeted anti-EV71 agent.

National Engineering Research Center For The Emergency Drug

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

University of Basel

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

TBA

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

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

Universit£

Inhibition of mTOR Kinase and Cancer Treatment.

Therachem Research Medilab (India)

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

Synthesis and anticancer activity of new dihydropyrimidinone derivatives.

Mansoura 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

Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent.

Astrazeneca

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

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

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

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

Shanghai Haiyan Pharmaceutical Technology

Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening.

University of Edinburgh

Identification of novel PI3K inhibitors through a scaffold hopping strategy.

Spanish National Cancer Research Centre (Cnio)

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

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

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

Novartis Institutes For Biomedical Research

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

Therachem Research Medilab (India)

Design, synthesis and biological evaluation of novel 3H-imidazole [4,5-b] pyridine derivatives as selective mTOR inhibitors.

China Pharmaceutical University

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

West China Hospital of Sichuan University

Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.

The Ohio State University

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

Astrazeneca

Highly Selective, Potent, and Oral mTOR Inhibitor for Treatment of Cancer as Autophagy Inducer.

Nankai University

Design, synthesis and SAR of new-di-substituted pyridopyrimidines as ATP-competitive dual PI3K?/mTOR inhibitors.

Temple University

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

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

Synthesis and characterization of metal complexes of heterocyclic sulfonamide as carbonic anhydrase inhibitors.

Dumlupinar University

Sulfapyridine-like benzenesulfonamide derivatives as inhibitors of carbonic anhydrase isoenzymes I, II and VI.

Ataturk University

Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols including natural products.

Atatürk University

Fluorobenzoyl dipeptidyl derivatives as inhibitors of the Fasciola hepatica cysteine protease cathepsin L1.

Dublin City University

Small-molecule WNK inhibition regulates cardiovascular and renal function.

Novartis Institutes

[125I]A-312110, a novel high-affinity 1,4-dihydropyridine ATP-sensitive K+ channel opener: characterization and pharmacology of binding.

Abbott Laboratories

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

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

Molecular and pharmacological characterization of muscarinic receptor subtypes in a rat parotid gland cell line: comparison with native parotid gland.

Creighton University

D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity.

University of Queensland Brisbane

Binding properties of the C-terminal domain of VIAF.

The Burnham Institute For Medical Research

MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells.

Gpc Biotech

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

University of California San Francisco

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

Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.

Pfizer

Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors.

Abbott Laboratories

Structure-activity relationships of HIV-1 PR inhibitors containing AHPBA--II. Modification of pyrrolidine ring at P1' proline.

Sankyo

Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors.

Upjohn