Staurosporine Analogs Via C-H Borylation

  • ACS Med Chem Lett. 2020 Oct 30;11(12):2441-2445. doi: 10.1021/acsmedchemlett.0c00420.
Kevin M Gayler  1 ,  Ke Kong  1 ,  Keighley Reisenauer  2 ,  Joseph H Taube  2 ,  John L Wood  1
Affiliations
  • 1. Department of Chemistry and Biochemistry, Baylor University, Waco, Texas 76798, United States.
  • 2. Department of Biology, Baylor University, Waco, Texas 76798, United States.
PMID: 33335665 DOI: 10.1021/acsmedchemlett.0c00420
Abstract

Staurosporine is among the most potent naturally occurring kinase inhibitors isolated to date and has served as a lead compound for numerous drug development efforts in several therapeutic areas. Herein we report that C-H borylation chemistry provides access to analogs of staurosporine that were previously inaccessible to medicinal chemists who, in the past four decades, have prepared over 1000 semisynthetic staurosporine analogs.