2. Academic Validation
  3. Novel pyridinyl and pyrimidinylcarbazole sulfonamides as antiproliferative agents

Novel pyridinyl and pyrimidinylcarbazole sulfonamides as antiproliferative agents

  • Bioorg Med Chem Lett. 2007 Mar 1;17(5):1193-6. doi: 10.1016/j.bmcl.2006.12.034.
Laixing Hu 1,  Zhuo-rong Li,  Yue-ming Wang,  Yanbin Wu,  Jian-Dong Jiang,  David W Boykin
Affiliations

Affiliation

  • 1 Department of Chemistry, Georgia State University, Atlanta, GA 30303-3083, USA.
PMID: 17197178 DOI: 10.1016/j.bmcl.2006.12.034
Abstract

A series of azaheterocyclic carbazole sulfonamides was synthesized and evaluated for antiproliferative activity. The most potent compounds N-(2,6-dimethoxypyridine-3-yl)-9-ethyl and 9-methylcarbazole-3-sulfonamide (13 and 14) gave significant cytotoxicity (IC50 = 122 and 101 nM). Compound 13 displayed submicromolar activities against seven human tumor cell lines. The SARs of this series of sulfonamides which includes the influence of azaheterocycle rings, sulfonamide linkage, and the carbazole ring are described.

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