Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR)

Journal of Medicinal Chemistry

Volumn 56, Issue 6, 2013, Pages 2218-2234

  Takeuchi, Craig S ^a   Kim, Byung Gyu ^a,b   Blazey, Charles M ^a   Ma, Sunghoon ^a   Johnson, Henry W B ^a   Anand, Neel K ^a   Arcalas, Arlyn ^a   Baik, Tae Gon ^a   Buhr, Chris A ^a   Cannoy, Jonah ^a   Epshteyn, Sergey ^a   Joshi, Anagha ^a   Lara, Katherine ^a   Lee, Matthew S ^a   Wang, Longcheng ^a   Leahy, James W ^a,c   Nuss, John M ^a   Aay, Naing ^a   Aoyama, Ron ^a   Foster, Paul ^a   Lee, Jae ^a   Lehoux, Isabelle ^a   Munagala, Narsimha ^a   Plonowski, Arthur ^a   Rajan, Sharmila ^a   Woolfrey, John ^a   Yamaguchi, Kyoko ^a   Lamb, Peter ^a   Miller, Nicole ^a   more..

^a EXELIXIS INC   (United States)

^b Asan Institute for Life Sciences   (South Korea)

^c UNIVERSITY OF SOUTH FLORIDA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

[7 (6 AMINOPYRIDIN 3 YL) 2,3 DIHYDROBENZ[F ][1,4]OXAZEPIN 4(5H) YL][3 FLUORO 2 METHYL 4 (METHYLSULFONYL)PHENYL] METHANONE; ANTINEOPLASTIC AGENT; DIBENZOXAZEPINE DERIVATIVE; MAMMALIAN TARGET OF RAPAMYCIN COMPLEX 1; MAMMALIAN TARGET OF RAPAMYCIN COMPLEX 2; MAMMALIAN TARGET OF RAPAMYCIN INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG COMPETITION; DRUG POTENCY; DRUG SELECTIVITY; ENZYME SUBSTRATE; HUMAN; HUMAN CELL; MOUSE; NONHUMAN; PROTEIN PHOSPHORYLATION; REACTION OPTIMIZATION; TUMOR XENOGRAFT;

ADENOSINE TRIPHOSPHATE; ADMINISTRATION, ORAL; ANIMALS; BENZOXAZINES; BINDING, COMPETITIVE; BIOLOGICAL AVAILABILITY; CELL LINE, TUMOR; DOGS; DRUG DISCOVERY; FEMALE; HUMANS; MALE; MICE; MODELS, MOLECULAR; PROTEIN CONFORMATION; PROTEIN KINASE INHIBITORS; RATS; SUBSTRATE SPECIFICITY; TOR SERINE-THREONINE KINASES;

EID: 84875706023     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm3007933     Document Type: Article

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