Design and synthesis of novel allosteric MEK inhibitor CH4987655 as an orally available anticancer agent

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 6, 2011, Pages 1795-1801

  Isshiki, Yoshiaki ^a   Kohchi, Yasunori ^a   Iikura, Hitoshi ^a   Matsubara, Yasuaki ^a   Asoh, Kohsuke ^a   Murata, Takeshi ^a   Kohchi, Masami ^a   Mizuguchi, Eisaku ^a   Tsujii, Shinji ^a   Hattori, Kazuo ^a   Miura, Takaaki ^a   Yoshimura, Yasushi ^a   Aida, Satoshi ^a   Miwa, Masanori ^a   Saitoh, Ryoichi ^a   Murao, Naoaki ^a   Okabe, Hisafumi ^a   Belunis, Charles ^b   Janson, Cheryl ^b   Lukacs, Christine ^b   Schück, Verena ^b   Shimma, Nobuo ^a   more..

^a CHUGAI PHARMACEUTICAL CO LTD   (Japan)

^b HOFFMANN LA ROCHE INC   (United States)

Author keywords

1,2 Oxazinan 3 one ring structure; Allosteric MEK inhibitor; Orally available anticancer agent

Indexed keywords

2 (2 CHLORO 4 IODOANILINO) N CYCLOPROPYLMETHOXY 3,4 DIFLUOROBENZAMIDE; ANTINEOPLASTIC AGENT; BENZAMIDE; CH 4858060; CH 4858061; CH 4987655; EVEROLIMUS; ISOXAZOLIDINONE; MITOGEN ACTIVATED PROTEIN KINASE; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; N (2,3 DIHYDROXYPROPOXY) 3,4 DIFLUORO 2 (2 FLUORO 4 IODOANILINO)BENZAMIDE; UNCLASSIFIED DRUG;

ALLOSTERISM; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BRAIN CANCER; CANCER COMBINATION CHEMOTHERAPY; CANCER INHIBITION; CENTRAL NERVOUS SYSTEM DISEASE; COLON CANCER; DRUG BLOOD LEVEL; DRUG DESIGN; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG MECHANISM; DRUG METABOLISM; DRUG SAFETY; DRUG STABILITY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TARGETING; ENZYME INHIBITION; HUMAN; IC 50; MALIGNANT NEOPLASTIC DISEASE; MAXIMUM TOLERATED DOSE; MONOTHERAPY; NONHUMAN; PERIPHERAL BLOOD MONONUCLEAR CELL; PHYSICAL CHEMISTRY; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION; SYNCOPE; TIME TO MAXIMUM PLASMA CONCENTRATION; VISUAL DISORDER;

ADMINISTRATION, ORAL; ALLOSTERIC REGULATION; ANTINEOPLASTIC AGENTS; BENZAMIDES; HUMANS; MAP KINASE KINASE KINASES; MODELS, MOLECULAR; OXAZINES; PROTEIN KINASE INHIBITORS;

EID: 79952360230     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.01.062     Document Type: Article

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