Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2- ones as potent and selective mTOR kinase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 22, 2011, Pages 6793-6799

  Mortensen, Deborah S ^a   Perrin Ninkovic, Sophie M ^a   Harris, Roy ^a   Lee, Branden G S ^a   Shevlin, Graziella ^a   Hickman, Matt ^a   Khambatta, Gody ^a   Bisonette, Rene R ^a   Fultz, Kimberly E ^a   Sankar, Sabita ^a  

^a CELGENE CORPORATION   (United States)

Author keywords

Kinase inhibitors; Mammalian target of rapamycin; mTOR kinase; Oncology; PI3K Akt mTOR pathway

Indexed keywords

ANTINEOPLASTIC AGENT; IMIDAZO[4,5 B]PYRAZIN 2 ONE; IMIDAZOPYRAZINE DERIVATIVE; MAMMALIAN TARGET OF RAPAMYCIN COMPLEX 1; MAMMALIAN TARGET OF RAPAMYCIN COMPLEX 2; MAMMALIAN TARGET OF RAPAMYCIN INHIBITOR; PHOSPHATIDYLINOSITOL 3 KINASE; PROTEIN KINASE B; PROTEIN S6; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER CELL; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; ENZYME INHIBITION; PROSTATE CANCER; SIGNAL TRANSDUCTION;

ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; DRUG DISCOVERY; HUMANS; MODELS, MOLECULAR; NEOPLASMS; PHOSPHATIDYLINOSITOL 3-KINASES; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-AKT; PYRAZINES; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP; TOR SERINE-THREONINE KINASES;

MAMMALIA;

EID: 80054722427     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.09.035     Document Type: Article

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