Discovery of 1-(4-(4-Propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9- (quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1 H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer

Journal of Medicinal Chemistry

Volumn 53, Issue 19, 2010, Pages 7146-7155

  Liu, Qingsong ^a,b   Chang, Jae Won ^a,b   Wang, Jinhua ^a,b   Kang, Seong A ^c   Thoreen, Carson C ^a,b   Markhard, Andrew ^c   Hur, Wooyoung ^a,b   Zhang, Jianming ^a,b   Sim, Taebo ^a,b   Sabatini, David M ^c,d   Gray, Nathanael S ^a,b  

^a DANA FARBER CANCER INSTITUTE   (United States)

^b HARVARD MEDICAL SCHOOL   (United States)

^c WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCH   (United States)

^d MASSACHUSETTS INSTITUTE OF TECHNOLOGY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [4 (4 ACETYLPIPERAZIN 1 YL) 3 (TRIFLUOROMETHYL)PHENYL] 9 (QUINOLIN 3 YL)BENZO[H][1,6]NAPHTHYRIDIN 2(1H) ONE; 1 [4 (4 PROPIONYLPIPERAZIN 1 YL) 3 (TRIFLUOROMETHYL)PHENYL] 9 (QUINOLIN 3 YL)BENZO[H][1,6]NAPHTHYRIDIN 2(1H) ONE; 1 [4 [4 [(3,6' BIQUINOLIN) 4' YLAMINO] 2 (TRIFLUOROMETHYL)PHENYL]PIPERAZIN 1 YL]ETHANONE; MAMMALIAN TARGET OF RAPAMYCIN INHIBITOR; PHOSPHATIDYLINOSITOL 3 KINASE; PHOSPHOTRANSFERASE; PROTEIN KINASE; QUINOLONE DERIVATIVE; TORIN1; UNCLASSIFIED DRUG; 1-(4-(4-PROPIONYLPIPERAZIN-1-YL)-3-(TRIFLUOROMETHYL)PHENYL)-9-(QUINOLIN-3-YL)BENZO(H)(1,6)NAPHTHYRIDIN-2(1H)-ONE; ANTINEOPLASTIC AGENT; MTOR PROTEIN, HUMAN; MTOR PROTEIN, MOUSE; NAPHTHYRIDINE DERIVATIVE; PROTEIN SERINE THREONINE KINASE; SIGNAL PEPTIDE; TARGET OF RAPAMYCIN KINASE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CANCER CHEMOTHERAPY; CELL ACTIVITY; CELL GROWTH; CELL PROLIFERATION; CONTROLLED STUDY; DRUG BINDING; DRUG CLEARANCE; DRUG DETERMINATION; DRUG EFFICACY; DRUG HALF LIFE; DRUG SELECTIVITY; DRUG STRUCTURE; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; FEMALE; HUMAN; HUMAN CELL; IC 50; MALE; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; DRUG SCREENING; IN VITRO STUDY; LIVER MICROSOME; METABOLISM; NUDE MOUSE; PHOSPHORYLATION; SYNTHESIS;

1-PHOSPHATIDYLINOSITOL 3-KINASE; ANIMALS; ANTINEOPLASTIC AGENTS; HUMANS; INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS; MALE; MICE; MICE, NUDE; MICROSOMES, LIVER; MODELS, MOLECULAR; NAPHTHYRIDINES; PHOSPHORYLATION; PROTEIN-SERINE-THREONINE KINASES; STRUCTURE-ACTIVITY RELATIONSHIP; XENOGRAFT MODEL ANTITUMOR ASSAYS; IN VITRO TECHNIQUES; PHOSPHATIDYLINOSITOL 3-KINASES; TOR SERINE-THREONINE KINASES;

EID: 77957903550     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm101144f     Document Type: Article

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