title: Novel pyridinyl and pyrimidinylcarbazole sulfonamides as antiproliferative agents.
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.
authors.affiliation: Department of Chemistry, Georgia State University, Atlanta, GA 30303-3083, USA.
authors.forename: Laixing
authors.initials: L
authors.lastname: Hu
authors.forename: Zhuo-rong
authors.initials: ZR
authors.lastname: Li
authors.forename: Yue-ming
authors.initials: YM
authors.lastname: Wang
authors.forename: Yanbin
authors.initials: Y
authors.lastname: Wu
authors.forename: Jian-Dong
authors.initials: JD
authors.lastname: Jiang
authors.forename: David W
authors.initials: DW
authors.lastname: Boykin
mesh_terms: 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*
chemical_list: D000970:Antineoplastic Agents; D002227:Carbazoles; D011725:Pyridines; D011743:Pyrimidines; D013449:Sulfonamides