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

Mustapha Haddach Jerome Michaux Michael K Schwaebe Fabrice Pierre Sean E O'Brien Cosmin Borsan Joe Tran Nicholas Raffaele Suchitra Ravula Denis Drygin Adam Siddiqui-Jain Levan Darjania Ryan Stansfield Chris Proffitt Diwata Macalino Nicole Streiner Joshua Bliesath May Omori Jeffrey P Whitten Kenna Anderes

ACS Med Chem Lett

Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.

Published: February 2012

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.

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 Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4025662PMC
http://dx.doi.org/10.1021/ml200259qDOI Listing

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