Abstract
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.
MeSH terms
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Antimitotic Agents / chemical synthesis
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Antimitotic Agents / chemistry*
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Antimitotic Agents / pharmacology
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Carbazoles / chemical synthesis
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Carbazoles / chemistry*
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Carbazoles / pharmacology
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Cell Line, Tumor
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Colchicine / pharmacology
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Drug Screening Assays, Antitumor
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HSP90 Heat-Shock Proteins / metabolism
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Humans
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Indoles / chemical synthesis
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Indoles / chemistry*
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Indoles / pharmacology
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Tubulin / metabolism
Substances
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Antimitotic Agents
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Carbazoles
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HSP90 Heat-Shock Proteins
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Indoles
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Tubulin
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Colchicine