Novel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives

Bioorg Med Chem Lett. 1999 Aug 2;9(15):2279-82. doi: 10.1016/s0960-894x(99)00375-3.

Abstract

A series of beta-substituted polythiophene derivatives was synthesized through palladium-catalyzed coupling reaction. Their structure-protein kinase C (PKC) inhibitory activity relationship was studied. The carboxaldehyde and hydroxymethyl derivatives of alpha-terthiophene were potent PKC inhibitors (IC50 = 10(-7) M).

Publication types

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

MeSH terms

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

Substances

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