Modifications of the isonipecotic acid fragment of SNS-032: Analogs with improved permeability and lower efflux ratio

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• 作者：Junfa Fan ; Bruce Fahr ; David Stockett ; Erica Chan ; Sravanthi Cheeti ; Iana Serafimova ; Yafan Lu ; Phuongly Pham ; Duncan H. Walker ; Ute Hoch ; Ingrid C. Choong
• 关键词：CDK ; Cyclin ; SNS-032 ; Kinase
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 出版时间：1 December 2008
• 年：2008
• 卷：18
• 期：23
• 页码：6236-6239
• 全文大小：165 K

文摘

Modifications of the isonipecotic acid fragment of SNS-032 results in analogs which are more permeable and lower effluxed than SNS-032. The enantiomerically pure synthesis and the in vivo profile of analog 20 is described.