265 articles for thisTarget
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Article Title
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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
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
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
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.
Zhejiang University
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.
Takeda Pharmaceutical
Computer-aided design, synthesis, and biological evaluation of new indole-2-carboxamide derivatives as PI3Ka/EGFR inhibitors.
The University Of Jordan
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
Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIß.
University Of California
Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.
Novartis Institutes For Biomedical Research
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 Novel and Orally Bioavailable Inhibitors of PI3 Kinase Based on Indazole Substituted Morpholino-Triazines.
Sphaera Pharma
The Rational Design of Selective Benzoxazepin Inhibitors of thea-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).
Genentech
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 and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9.
The University Of Melbourne
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
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
Discovery of a 6-(pyridin-3-yl)benzo[d]thiazole template for optimization of hedgehog and PI3K/AKT/mTOR dual inhibitors.
Soochow University
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
Synthesis and evaluation of pyrrolotriazine based molecules as PI3 kinase inhibitors.
Sphaera Pharma
Molecular modeling based approach, synthesis, and cytotoxic activity of novel benzoin derivatives targeting phosphoinostide 3-kinase (PI3Ka).
Al-Zaytoonah University Of Jordan
Discovery of potent, selective small molecule inhibitors ofa-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIa).
Astrazeneca
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
Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115.
Celgene
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
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
Synthesis and antitumor activities evaluation of m-(4-morpholinoquinazolin-2-yl)benzamides in vitro and in vivo.
Xi'An Jiaotong 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
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
Design, synthesis and antiproliferative activity evaluation of m-(4-morpholinyl-1,3,5-triazin-2-yl)benzamides in vitro.
Xi'An Jiaotong University
6,7-Dihydrobenzo[f]benzo[4,5]imidazo[1,2-d][1,4]oxazepine derivatives as selective inhibitors of PI3Ka.
Nanjing University
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 and biological evaluation of potent and selective c-KIT(D816V) inhibitors.
Korea Advanced Institute Of Science And Technology (Kaist)
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
Structural basis for isoform selectivity in a class of benzothiazole inhibitors of phosphoinositide 3-kinase¿.
Vertex Pharmaceuticals
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
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents.
Shenyang Pharmaceutical University
Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors.
Universit£
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
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
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
Discovery and optimization of pyrimidone indoline amide PI3Kß inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
Sanofi
Crystal Structures of PI3K? Complexed with PI103 and Its Derivatives: New Directions for Inhibitors Design.
Shanghai Jiao Tong University
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
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.
Novartis Institutes For Biomedical Research
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
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
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
Celgene
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
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
Synthesis and biological evaluation of novel coumarin-pyrazoline hybrids endowed with phenylsulfonyl moiety as antitumor agents.
Cairo University
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
Lead optimization of a dihydropyrrolopyrimidine inhibitor against phosphoinositide 3-kinase (PI3K) to improve the phenol glucuronic acid conjugation.
Chugai Pharmaceutical
Identification of ETP-46321, a potent and orally bioavailable PI3Ka,d inhibitor.
Spanish National Cancer Research Centre (Cnio)
Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors.
TBA
Discovery and optimization of a series of 2-aminothiazole-oxazoles as potent phosphoinositide 3-kinase¿ inhibitors.
Taisho Pharmaceutical
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
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
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
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
Design, synthesis, and evaluation of 3,5-disubstituted 7-azaindoles as Trk inhibitors with anticancer and antiangiogenic activities.
Korea Advanced Institute Of Science And Technology (Kaist)
Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Ka inhibitors.
Universit£
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
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)
Discovery of MEK/PI3K dual inhibitor via structure-based virtual screening.
Sejong University
Structure-based optimization of aminopyridines as PKC¿ inhibitors.
Vertex Pharmaceuticals
Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor.
Astrazeneca
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.
Ambit Biosciences
Discovery of novel 2-piperidinol-3-(arylsulfonyl)quinoxalines as phosphoinositide 3-kinasea (PI3Ka) inhibitors.
Zhejiang 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
Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity.
TBA
Discovery of new azaindole-based PI3Ka inhibitors: apoptotic and antiangiogenic effect on cancer cells.
Institute Of Science And Technology (Kaist)
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
Optimization of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine inhibitors of IGF-1R: elimination of an acid-mediated decomposition pathway.
Glaxosmithkline
Exploring the PI3K alpha and gamma binding sites with 2,6-disubstituted isonicotinic derivatives.
University Of Cincinnati
Design and synthesis of novel furoquinoline based inhibitors of multiple targets in the PI3K/Akt-mTOR pathway.
Nicholas Piramal Research Centre
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University Of Oxford
Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.
Novartis Institute For Biomedical Research
Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors.
Astellas Pharma
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
Imidazo[1,2-a]pyrazines as novel PI3K inhibitors.
Spanish National Cancer Research Centre (Cnio)
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
Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2-ones as potent and selective mTOR kinase inhibitors.
Celgene
Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
Chinese Academy Of Sciences
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 new aminopyrimidine-based phosphoinositide 3-kinase beta (PI3Kß) inhibitors with selectivity over PI3Ka.
Institute Of Science And Technology (Kaist)
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
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
Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl)quinoxalines as PI3Ka inhibitors.
Zhejiang University
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
Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment.
Sanofi-Aventis
Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability.
Dana-Farber Cancer Institute
Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.
Amgen
Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis.
Korea Advanced Institute Of Science And Technology
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
Structure-based virtual screening approach to the discovery of phosphoinositide 3-kinase alpha inhibitors.
Sejong University
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
DNA-dependent protein kinase (DNA-PK) inhibitors: structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain.
Newcastle University
Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements.
The Institute Of Cancer Research
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
Synthesis of phosphatidylinositol 3-kinase (PI3K) inhibitory analogues of the sponge meroterpenoid liphagal.
University Of British Columbia
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
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
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
Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors.
Wyeth Research
Novel benzofuran-3-one indole inhibitors of PI3 kinase-alpha and the mammalian target of rapamycin: hit to lead studies.
Wyeth Research
Triazines incorporating (R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kalpha.
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
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
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.
Wyeth Research
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
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
4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.
Wyeth Research
Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.
Amgen
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
Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one.
Stony Brook University
Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors.
University Of Auckland
Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.
Serono Pharmaceutical Research Institute
Synthesis of fluorescent derivatives of wortmannin and demethoxyviridin as probes for phosphatidylinositol 3-kinase.
State University Of New York-Esf
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
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.
University Of Newcastle
3-Deoxy-3-substituted-D-myo-inositol imidazolyl ether lipid phosphates and carbonate as inhibitors of the phosphatidylinositol 3-kinase pathway and cancer cell growth.
Georgetown University Medical Center
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
Synthesis and activity of amides of tripeptides as potential urokinase inhibitors.
Medical University Of Bialystok
Fluorobenzoyl dipeptidyl derivatives as inhibitors of the Fasciola hepatica cysteine protease cathepsin L1.
Dublin City University
Ellagitannin and flavonoid constituents from Agrimonia pilosa Ledeb. with their protein tyrosine phosphatase and acetylcholinesterase inhibitory activities
Catholic University Of Daegu
Rational design, synthesis, pharmacophore modeling, and docking studies for identification of novel potent DNA-PK inhibitors
Taibah University
Kinetics and inhibition of nicotinamidase from Mycobacterium tuberculosis.
Albert Einstein College Of Medicine
[125I]A-312110, a novel high-affinity 1,4-dihydropyridine ATP-sensitive K+ channel opener: characterization and pharmacology of binding.
Abbott Laboratories
Receptor occupancy and adenylate cyclase activation in AR 4-2J rat pancreatic acinar cell membranes by analogs of pituitary adenylate cyclase-activating peptides amino-terminally shortened or modified at position 1, 2, 3, 20, or 21.
Universit&Acute
Inhibitors of tubulin assembly identified through screening a compound library.
The Ohio State University
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
University Of California San Francisco
Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase.
Wyeth Research
ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin: Design and Synthesis of Highly Potent and Selective Pyrazolopyrimidines
Wyeth Research
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
Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.
Wyeth Research