Novel protein kinase C inhibitors: alpha-terthiophene derivatives

Bioorg Med Chem Lett. 1998 Oct 6;8(19):2695-8. doi: 10.1016/s0960-894x(98)00468-5.

Abstract

A series of alpha-terthiophene derivatives were prepared and their protein kinase C inhibitory activity were evaluated. The aldehyde derivatives were most potent inhibitors (IC50 < 1 microM). alpha-Terthiophene monoaldehyde was inactive in the inhibitions of protein kinase A, mitogen activated protein kinase and protein tyrosine kinase.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • Protein Kinase C / antagonists & inhibitors*
  • Structure-Activity Relationship
  • Thiophenes / chemical synthesis*
  • Thiophenes / pharmacology*

Substances

  • Enzyme Inhibitors
  • Thiophenes
  • alpha-terthienyl
  • Protein Kinase C