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

  • Bioorg Med Chem Lett. 2008 Dec 1;18(23):6236-9. doi: 10.1016/j.bmcl.2008.09.099.
Junfa Fan  1 ,  Bruce Fahr ,  David Stockett ,  Erica Chan ,  Sravanthi Cheeti ,  Iana Serafimova ,  Yafan Lu ,  Phuongly Pham ,  Duncan H Walker ,  Ute Hoch ,  Ingrid C Choong
Affiliations
  • 1. Sunesis Pharmaceuticals, 341 Oyster Point Blvd, South San Francisco, CA 94080, USA. [email protected]
PMID: 18926699 DOI: 10.1016/j.bmcl.2008.09.099
Abstract

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.