Novel pyridinyl and pyrimidinylcarbazole sulfonamides as antiproliferative agents

Carbazole sulfonamides II showed potent antiproliferative activity. 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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-03, Vol.17 (5), p.1193-1196
Main Authors: Hu, Laixing, Li, Zhuo-rong, Wang, Yue-ming, Wu, Yanbin, Jiang, Jian-Dong, Boykin, David W.
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Antiproliferative agents
Biological and medical sciences
Carbazoles
Cell Line, Tumor
Drug Screening Assays, Antitumor
General aspects
Humans
Inhibitory Concentration 50
Medical sciences
Pharmacology. Drug treatments
Pyridines
Pyrimidines
Structure-Activity Relationship
Sulfonamides
Sulfonamides - chemical synthesis
Sulfonamides - chemistry
Sulfonamides - pharmacology
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Summary:Carbazole sulfonamides II showed potent antiproliferative activity. 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 (IC 50 = 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.12.034