Synthesis of amide and urea derivatives of benzothiazole as Raf-1 inhibitor

Eur J Med Chem. 2008 Jul;43(7):1519-24. doi: 10.1016/j.ejmech.2007.10.008. Epub 2007 Oct 11.

Abstract

A series of amide and urea derivatives of benzothiazole have been synthesized and evaluated for their antiproliferative profile in human SK-Hep-1 (liver), MDA-MB-231 (breast), and NUGC-3 (gastric) cell lines. Among them, compounds 1-2, 16-18, 23, and 25-26 had potent to moderate inhibitory activities. Further these compounds were investigated for their ability to inhibit Raf-1 activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis*
  • Benzothiazoles / chemical synthesis
  • Benzothiazoles / chemistry
  • Benzothiazoles / pharmacology*
  • Cell Line, Tumor
  • Humans
  • Magnetic Resonance Spectroscopy
  • Protein Kinase Inhibitors / chemical synthesis
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology*
  • Proto-Oncogene Proteins c-raf / antagonists & inhibitors*
  • Spectrometry, Mass, Electrospray Ionization
  • Urea / chemical synthesis*

Substances

  • Amides
  • Benzothiazoles
  • Protein Kinase Inhibitors
  • Urea
  • Proto-Oncogene Proteins c-raf