Merck
  • Home
  • Search Results
  • Novel potent antimitotic heterocyclic ketones: synthesis, antiproliferative activity, and structure-activity relationships.

Novel potent antimitotic heterocyclic ketones: synthesis, antiproliferative activity, and structure-activity relationships.

Bioorganic & medicinal chemistry letters (2007-05-08)
Laixing Hu, Jian-dong Jiang, Jinrong Qu, Yan Li, Jie Jin, Zhuo-rong Li, David W Boykin
ABSTRACT

We report the synthesis, antiproliferative activity, and SAR of novel heterocyclic ketones derived from carbazole sulfonamides. Most of the heterocyclic ketones showed strong cytotoxicities. (N-1-Methylindole-5-yl)-(3,4,5-trimethoxyphenyl)-methanone 8b gave the most potent cytotoxicity (9.2-26 nM) against seven human tumor cell lines. The mechanism of action of the heterocyclic ketones appears to involve targeting of tubulin, similar to that of CA-4 and different from the carbazole sulfonamides.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Podophyllotoxin