Synthesis of selenophene derivatives as novel CHK1 inhibitors

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5065-8. doi: 10.1016/j.bmcl.2010.07.034. Epub 2010 Jul 13.

Abstract

A series of selenophene derivatives 3 were synthesized as potential CHK1 inhibitors. The effects of substitution on the 4'- or 5'-position of selenophene moiety and shifting the hydroxyl group position on C6- phenolic ring of oxindole were explored. This study led to the discovery of the most potent CHK1 inhibitors 29-33 and 39-43, which had IC(50) values in the subnanomolar range.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Checkpoint Kinase 1
  • Protein Kinase Inhibitors / chemical synthesis*
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinases / drug effects*
  • Selenium Compounds / chemical synthesis*
  • Selenium Compounds / pharmacology

Substances

  • Protein Kinase Inhibitors
  • Selenium Compounds
  • Protein Kinases
  • Checkpoint Kinase 1