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

  作者 HADDACH MUSTAPHA; MICHAUX JEROME; SCHWAEBE MICHAEL K; PIERRE FABRICE; OBRIEN SEAN E; BORSAN COSMIN; TRAN JOE; RAFFAELE NICHOLAS; RAVULA SUCHITRA; DRYGIN DENIS; SIDDIQUIJAIN ADAM; DARJANIA LEVAN; STANSFIELD RYAN; PROFFITT CHRIS; MACALINO DIWATA; STREINER NICOLE; BLIESATH JOSHUA; OMORI MAY; WHITTEN JEFFREY P; ANDERES KENNA; RICE WILLIAM G; RYCKMAN DAVID M  
  选自 期刊  ACS Medicinal Chemistry Letters;  卷期  2012年3-2;  页码  135-139  
  关联知识点  
 

[摘要]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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