Novel pyridinyl and pyrimidinylcarbazole sulfonamides as antiproliferative agents.
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.
Hu
Laixing
L
Department of Chemistry, Georgia State University, Atlanta, GA 30303-3083, USA.
Li
Zhuo-rong
ZR
Wang
Yue-ming
YM
Wu
Yanbin
Y
Jiang
Jian-Dong
JD
Boykin
David W
DW
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002227:Carbazoles; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D011725:Pyridines; D011743:Pyrimidines; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000970:Antineoplastic Agents; D002227:Carbazoles; D011725:Pyridines; D011743:Pyrimidines; D013449:Sulfonamides