Novel carbazole and acyl-indole antimitotics

Bioorg Med Chem Lett. 2009 Jun 1;19(11):3078-80. doi: 10.1016/j.bmcl.2009.04.010. Epub 2009 Apr 9.

Abstract

In the course of our Heat Shock 90 program, certain carbazole compounds were identified which had an off-target antiproliferative activity. To understand the off-target activity, we studied one analog with strong activity. We discovered that it had an effect on tubulin polymerization kinetics and was competitive with colchicine. Additional analogs were made, and a number of potent compounds were identified.

MeSH terms

  • Antimitotic Agents / chemical synthesis
  • Antimitotic Agents / chemistry*
  • Antimitotic Agents / pharmacology
  • Carbazoles / chemical synthesis
  • Carbazoles / chemistry*
  • Carbazoles / pharmacology
  • Cell Line, Tumor
  • Colchicine / pharmacology
  • Drug Screening Assays, Antitumor
  • HSP90 Heat-Shock Proteins / metabolism
  • Humans
  • Indoles / chemical synthesis
  • Indoles / chemistry*
  • Indoles / pharmacology
  • Tubulin / metabolism

Substances

  • Antimitotic Agents
  • Carbazoles
  • HSP90 Heat-Shock Proteins
  • Indoles
  • Tubulin
  • Colchicine