Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115

Journal of Medicinal Chemistry

Volumn 58, Issue 14, 2015, Pages 5599-5608

  Mortensen, Deborah S ^a   Perrin Ninkovic, Sophie M ^a   Shevlin, Graziella ^a   Elsner, Jan ^a   Zhao, Jingjing ^a   Whitefield, Brandon ^a   Tehrani, Lida ^a   Sapienza, John ^a   Riggs, Jennifer R ^a   Parnes, Jason S ^a   Papa, Patrick ^a   Packard, Garrick ^a   Lee, Branden G S ^a   Harris, Roy ^a   Correa, Matthew ^a   Bahmanyar, Sogole ^a   Richardson, Samantha J ^a   Peng, Sophie X ^a   Leisten, Jim ^a   Khambatta, Godrej ^a   Hickman, Matt ^a   Gamez, James C ^a   Bisonette, René R ^a   Apuy, Julius ^a   Cathers, Brian E ^a   Canan, Stacie S ^a   Moghaddam, Mehran F ^a   Raymon, Heather K ^a   Worland, Peter ^a   Narla, Rama Krishna ^a   Fultz, Kimberly E ^a   Sankar, Sabita ^a   more..

^a CELGENE CORPORATION   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CC 115; MAMMALIAN TARGET OF RAPAMYCIN INHIBITOR; PYRAZINE DERIVATIVE; TRIAZOLE DERIVATIVE; UNCLASSIFIED DRUG; 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL)PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-B)PYRAZIN-2(1H)-ONE; PROTEIN KINASE INHIBITOR; TARGET OF RAPAMYCIN KINASE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CANCER CELL LINE; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFICACY; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; MALE; NONHUMAN; RAT; SIGNAL TRANSDUCTION; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION; TUMOR XENOGRAFT; ANIMAL; ANTAGONISTS AND INHIBITORS; CELL PROLIFERATION; CHEMISTRY; DRUG DESIGN; DRUG EFFECTS; DRUG SCREENING; METABOLISM; MOLECULAR DOCKING; PROTEIN CONFORMATION; TUMOR CELL LINE;

ANIMALS; CELL LINE, TUMOR; CELL PROLIFERATION; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; HUMANS; MOLECULAR DOCKING SIMULATION; PROTEIN CONFORMATION; PROTEIN KINASE INHIBITORS; PYRAZINES; RATS; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP; TOR SERINE-THREONINE KINASES; TRIAZOLES; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84937446170     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b00627     Document Type: Article

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