Conformationally restricted analogs of Combretastatin A-4 derived from SU5416

A series of compounds originally derived from the vascular endothelial growth factor receptor tyrosine kinase inhibitor, SU5416, was synthesized and evaluated. The most potent compound in this series, compound 7, structurally resembles the potent anti-microtubule agent Combretastatin A-4, inhibited...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-12, Vol.15 (24), p.5382-5385
Hauptverfasser:	Li, Pui-Kai, Xiao, Zili, Hu, Zhigen, Pandit, Bulbul, Sun, Yanjun, Sackett, Dan L., Werbovetz, Karl, Lewis, Andrew, Johnsamuel, Jayasekar
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic agents Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Biological and medical sciences Brain - cytology Brain - drug effects Brain - metabolism Cell Division - drug effects General aspects Indoles - chemistry Medical sciences Models, Molecular Molecular Conformation Pharmacology. Drug treatments Pyrroles - chemistry Stilbenes - chemistry Swine Tubulin - drug effects Tubulin - metabolism
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Beschreibung
Zusammenfassung:	A series of compounds originally derived from the vascular endothelial growth factor receptor tyrosine kinase inhibitor, SU5416, was synthesized and evaluated. The most potent compound in this series, compound 7, 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 IC 50 values in low to subnanomolar range.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.09.001