Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[ h ][1,6]naphthyridin-2(1 H)-one (torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer

Journal of Medicinal Chemistry

Volumn 54, Issue 5, 2011, Pages 1473-1480

  Liu, Qingsong ^a,b   Wang, Jinhua ^a,b   Kang, Seong A ^c   Thoreen, Carson C ^a,b   Hur, Wooyoung ^a,b   Ahmed, Tausif ^d   Sabatini, David M ^c,e,f   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 Sai Advantium Pharma Ltd   (India)

^e MASSACHUSETTS INSTITUTE OF TECHNOLOGY   (United States)

^f KOCH INSTITUTE FOR INTEGRATIVE CANCER RESEARCH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [4 (4 PROPIONYLPIPERAZIN 1 YL) 3 (TRIFLUOROMETHYL)PHENYL] 9 (QUINOLIN 3 YL)BENZO[H][1,6]NAPHTHYRIDIN 2(1H) ONE; 9 (6 AMINOPYRIDIN 3 YL) 1 [3 (TRIFLUOROMETHYL)PHENYL]BENZO[H][1,6]NAPHTHYRIDIN 2(1H) ONE; MAMMALIAN TARGET OF RAPAMYCIN; MAMMALIAN TARGET OF RAPAMYCIN INHIBITOR; PHOSPHATIDYLINOSITOL 3 KINASE; PROTEIN SERINE THREONINE KINASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CANCER CHEMOTHERAPY; DRUG BIOAVAILABILITY; DRUG METABOLISM; DRUG PROTEIN BINDING; DRUG SCREENING; DRUG SELECTIVITY; ENZYME INHIBITION; MALE; MOUSE; NONHUMAN;

ADMINISTRATION, ORAL; AMINOPYRIDINES; ANIMALS; ANTINEOPLASTIC AGENTS; BIOLOGICAL AVAILABILITY; DRUG STABILITY; MALE; MICE; MICE, INBRED C57BL; MICROSOMES, LIVER; MODELS, MOLECULAR; NAPHTHYRIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; TOR SERINE-THREONINE KINASES;

EID: 79952265072     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm101520v     Document Type: Article

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