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Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.

ABSTRACT: Structure-activity relationship analysis in a series of 3-(5-((2-oxoindolin-3-ylidene)methyl)furan-2-yl)amides identified compound 13, a pan-Pim kinases inhibitor with excellent biochemical potency and kinase selectivity. Compound 13 exhibited in vitro synergy with chemotherapeutics and robust in vivo efficacy in two Pim kinases driven tumor models.

SUBMITTER: Haddach M

PROVIDER: S-EPMC4025662 | biostudies-literature | 2012 Feb

REPOSITORIES: biostudies-literature

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Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.

Haddach Mustapha M Michaux Jerome J Schwaebe Michael K MK Pierre Fabrice F O'Brien Sean E SE Borsan Cosmin C Tran Joe J Raffaele Nicholas N Ravula Suchitra S Drygin Denis D Siddiqui-Jain Adam A Darjania Levan L Stansfield Ryan R Proffitt Chris C Macalino Diwata D Streiner Nicole N Bliesath Joshua J Omori May M Whitten Jeffrey P JP Anderes Kenna K Rice William G WG Ryckman David M DM

ACS medicinal chemistry letters 20111227 2

Structure-activity relationship analysis in a series of 3-(5-((2-oxoindolin-3-ylidene)methyl)furan-2-yl)amides identified compound 13, a pan-Pim kinases inhibitor with excellent biochemical potency and kinase selectivity. Compound 13 exhibited in vitro synergy with chemotherapeutics and robust in vivo efficacy in two Pim kinases driven tumor models. ...[more]

PMID: 24900437

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