Synthesis and SAR of 2-arylbenzoxazoles, benzothiazoles and benzimidazoles as inhibitors of lysophosphatidic acid acyltransferase-beta

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1455-9. doi: 10.1016/j.bmcl.2004.01.023.

Abstract

2-Arylbenzoxazoles, benzothiazoles and benzimidazoles were identified as new classes of potent, isoform specific inhibitors of lysophosphatidic acid acyltransferase-beta (LPAAT-beta). Effects of selected inhibitors on proliferation of tumor cells in vitro were investigated.

MeSH terms

  • Acyltransferases / antagonists & inhibitors*
  • Acyltransferases / metabolism
  • Benzimidazoles / chemistry*
  • Benzimidazoles / pharmacology
  • Benzothiazoles
  • Benzoxazoles / chemistry*
  • Benzoxazoles / pharmacology
  • Cell Line, Tumor
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Structure-Activity Relationship
  • Thiazoles / chemistry*
  • Thiazoles / pharmacology

Substances

  • Benzimidazoles
  • Benzothiazoles
  • Benzoxazoles
  • Enzyme Inhibitors
  • Thiazoles
  • Acyltransferases
  • 2-acylglycerophosphate acyltransferase
  • benzothiazole