Synthesis and Structure−Activity Relationships of Carbazole Sulfonamides as a Novel Class of Antimitotic Agents Against Solid Tumors

Two series of carbazole sulfonamides related to Combretastatin A4 (1) were synthesized and evaluated for antiproliferative activity. Thirteen of the 26 new sulfonamides exhibited IC50 values of

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Bibliographic Details
Published in:Journal of medicinal chemistry 2006-10, Vol.49 (21), p.6273-6282
Main Authors: Hu, Laixing, Li, Zhuo-rong, Li, Yan, Qu, Jinrong, Ling, Yi-He, Jiang, Jian-dong, Boykin, David W
Format: Article
Language:English
Subjects:
Animals
Antimitotic Agents - chemical synthesis
Antimitotic Agents - chemistry
Antimitotic Agents - pharmacology
Antineoplastic agents
Apoptosis
Biological and medical sciences
Breast Neoplasms - drug therapy
Carbazoles - chemical synthesis
Carbazoles - chemistry
Carbazoles - pharmacology
Carcinoma, Hepatocellular - drug therapy
Cell Division - drug effects
Cell Line, Tumor
Drug Screening Assays, Antitumor
Female
General aspects
Humans
Liver Neoplasms - drug therapy
Medical sciences
Mice
Mice, Nude
Neoplasm Transplantation
Pharmacology. Drug treatments
Phosphorylation
Proto-Oncogene Proteins c-bcl-2 - metabolism
Structure-Activity Relationship
Sulfonamides - chemical synthesis
Sulfonamides - chemistry
Sulfonamides - pharmacology
Transplantation, Heterologous
Tumor Suppressor Protein p53 - biosynthesis
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Description
Summary:Two series of carbazole sulfonamides related to Combretastatin A4 (1) were synthesized and evaluated for antiproliferative activity. Thirteen of the 26 new sulfonamides exhibited IC50 values of
ISSN:0022-2623
1520-4804
DOI:10.1021/jm060546h