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

Journal of Medicinal Chemistry

Volumn 54, Issue 9, 2011, Pages 3426-3435

  Cohen, Frederick ^a   Bergeron, Philippe ^a   Blackwood, Elizabeth ^a   Bowman, Krista K ^a   Chen, Huifen ^a   Dipasquale, Antonio G ^a   Epler, Jennifer A ^a   Koehler, Michael F T ^a   Lau, Kevin ^a   Lewis, Cristina ^a   Liu, Lichuan ^a   Ly, Cuong Q ^a   Malek, Shiva ^a   Nonomiya, Jim ^a   Ortwine, Daniel F ^a   Pei, Zhonghua ^a   Robarge, Kirk D ^a   Sideris, Steve ^a   Trinh, Lan ^a   Truong, Tom ^a   Wu, Jiansheng ^b   Zhao, Xianrui ^a   Lyssikatos, Joseph P ^a   more..

^a GENENTECH INC   (United States)

^b UNIVERSITY OF CALIFORNIA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [4 [7,7 DIMETHYL 4 (3 METHYLMORPHOLINO) 5,7 DIHYDROFURO[3,4 D]PYRIMIDIN 2 YL]PHENYL] 3 ETHYLUREA; ETHYL 3 [4 [7 (2 HYDROXYETHYL) 7 METHYL-4 (3 METHYLMORPHOLINO) 5,7 DIHYDROFURO[3,4 D]PYRIMIDIN 2 YL]PHENYL]UREA; MAMMALIAN TARGET OF RAPAMYCIN; MAMMALIAN TARGET OF RAPAMYCIN INHIBITOR; PHOSPHATIDYLINOSITOL 3 KINASE; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CELL PROLIFERATION; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG HALF LIFE; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; FEMALE; HUMAN; HUMAN CELL; IC 50; MALE; MOLECULAR MODEL; MOUSE; NONHUMAN;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; BIOLOGICAL AVAILABILITY; CELL LINE, TUMOR; DRUG SCREENING ASSAYS, ANTITUMOR; DRUG STABILITY; FURANS; HUMANS; MICE; MICE, NUDE; MODELS, MOLECULAR; NEOPLASM TRANSPLANTATION; PHOSPHATIDYLINOSITOL 3-KINASES; PYRIMIDINES; RATS; SPECIES SPECIFICITY; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TOR SERINE-THREONINE KINASES; TRANSPLANTATION, HETEROLOGOUS;

EID: 79955809222     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm200215y     Document Type: Article

References (19)

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