Design, synthesis and biological studies of novel tubulin inhibitors

A series of compounds originally derived from the vascular endothelial growth factor receptor tyrosine kinase inhibitor, SU5416, were synthesized and evaluated. The most potent compound in this series, compound 3, which structurally resembles the potent anti-microtubule agent combretastatin A-4, inh...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2013-08, Vol.23 (15), p.4465-4468
Hauptverfasser: Sun, Yanjun, Pandit, Bulbul, Chettiar, Somsundaram N., Etter, Jonathan P., Lewis, Andrew, Johnsamuel, Jayasekar, Li, Pui-Kai
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container_end_page 4468
container_issue 15
container_start_page 4465
container_title Bioorganic & medicinal chemistry letters
container_volume 23
creator Sun, Yanjun
Pandit, Bulbul
Chettiar, Somsundaram N.
Etter, Jonathan P.
Lewis, Andrew
Johnsamuel, Jayasekar
Li, Pui-Kai
description A series of compounds originally derived from the vascular endothelial growth factor receptor tyrosine kinase inhibitor, SU5416, were synthesized and evaluated. The most potent compound in this series, compound 3, which structurally resembles the potent anti-microtubule agent combretastatin A-4, inhibited tubulin polymerization and showed potent growth inhibitory activities on both prostate and breast cancer lines with IC50 values in the low nanomolar range.
doi_str_mv 10.1016/j.bmcl.2013.04.078
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subjects Anti-microtubule agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Bibenzyls - pharmacology
Breast cancer
Cell Line, Tumor
Cell Proliferation - drug effects
Drug Design
Humans
Polymerization - drug effects
Tubulin - chemistry
Tubulin - metabolism
Tubulin inhibitors
Tubulin Modulators - chemical synthesis
Tubulin Modulators - chemistry
Tubulin Modulators - pharmacology
title Design, synthesis and biological studies of novel tubulin inhibitors
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