Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor
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- 作者：Mustapha Haddach ; Jerome Michaux ; Michael K. Schwaebe ; Fabrice Pierre ; Sean E. O鈥橞rien ; 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 ; William G. Rice ; David M. Ryckman
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2012
- 出版时间：February 9, 2012
- 年：2012
- 卷：3
- 期：2
- 页码：135-139
- 全文大小：259K
- 年卷期：v.3,no.2(February 9, 2012)
- ISSN：1948-5875
文摘
Structure鈥揳ctivity 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.