Novel carbazole and acyl-indole antimitotics

In the course of our Heat Shock 90 program, certain carbazole compounds were identified which had an off-target antiproliferative activity. To understand the off-target activity, we studied one analog with strong activity. We discovered that it had an effect on tubulin polymerization kinetics and wa...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-06, Vol.19 (11), p.3078-3080
Main Authors: Barta, Thomas E., Barabasz, Amy F., Foley, Briana E., Geng, Lifeng, Hall, Steven E., Hanson, Gunnar J., Jenks, Matthew, Ma, Wei, Rice, John W., Veal, James
Format: Article
Language:English
Subjects:
Antimitotic
Antimitotic Agents - chemical synthesis
Antimitotic Agents - chemistry
Antimitotic Agents - pharmacology
Antineoplastic agents
Antiproliferative
Biological and medical sciences
Cancer
Carbazole
Carbazoles - chemical synthesis
Carbazoles - chemistry
Carbazoles - pharmacology
Cell Line, Tumor
Colchicine
Colchicine - pharmacology
Drug Screening Assays, Antitumor
General aspects
HSP90 Heat-Shock Proteins - metabolism
Humans
Indoles - chemical synthesis
Indoles - chemistry
Indoles - pharmacology
Medical sciences
Oncology
Pharmacology. Drug treatments
Tubulin
Tubulin - metabolism
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Summary:In the course of our Heat Shock 90 program, certain carbazole compounds were identified which had an off-target antiproliferative activity. To understand the off-target activity, we studied one analog with strong activity. We discovered that it had an effect on tubulin polymerization kinetics and was competitive with colchicine. Additional analogs were made, and a number of potent compounds were identified.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.04.010