2. Academic Validation
  3. Novel potent antimitotic heterocyclic ketones: synthesis, antiproliferative activity, and structure-activity relationships

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

  • Bioorg Med Chem Lett. 2007 Jul 1;17(13):3613-7. doi: 10.1016/j.bmcl.2007.04.048.
Laixing Hu 1,  Jian-dong Jiang,  Jinrong Qu,  Yan Li,  Jie Jin,  Zhuo-rong Li,  David W Boykin
Affiliations

Affiliation

  • 1 Department of Chemistry, Georgia State University, Atlanta, GA 30303-3083, USA.
PMID: 17482458 DOI: 10.1016/j.bmcl.2007.04.048
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.

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