Biological evaluation of novel 6-Arylbenzimidazo[1,2-c]quinazoline derivatives as inhibitors of LPS-induced TNF-alpha secretion

Biol Res. 2008;41(1):43-50. Epub 2008 Aug 21.

Abstract

This study describes the effect of novel 6-Arylbenzimidazo[1,2-c]quinazoline derivatives as tumor necrosis factor alpha (TNF-alpha) production inhibitors. The newly synthesized compounds were tested for their in vitro ability to inhibit the lipolysaccharide (LPS) induced TNF-alpha secretion in the human promyelocytic cell line HL-60. The compound 6-Phenyl-benzimidazo[1,2-c]quinazoline, coded as Gl, resulted as the most potent inhibitor and with no significant cytotoxic activity. Thus, 6-Arylbenzimidazo[1,2-c]quinazoline derivatives may have a potential as anti-inflammatory agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology*
  • HL-60 Cells
  • Humans
  • Lipopolysaccharides / pharmacology
  • Quinazolines / chemistry
  • Quinazolines / pharmacology*
  • RNA, Messenger / drug effects
  • RNA, Messenger / metabolism
  • Tetradecanoylphorbol Acetate / analogs & derivatives
  • Tetradecanoylphorbol Acetate / pharmacology
  • Tumor Necrosis Factor-alpha / antagonists & inhibitors*
  • Tumor Necrosis Factor-alpha / biosynthesis

Substances

  • Anti-Inflammatory Agents
  • Lipopolysaccharides
  • Quinazolines
  • RNA, Messenger
  • Tumor Necrosis Factor-alpha
  • 4-O-methyl-12-O-tetradecanoylphorbol 13-acetate
  • Tetradecanoylphorbol Acetate