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
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container_end_page 5385
container_issue 24
container_start_page 5382
container_title Bioorganic & medicinal chemistry letters
container_volume 15
creator Li, Pui-Kai
Xiao, Zili
Hu, Zhigen
Pandit, Bulbul
Sun, Yanjun
Sackett, Dan L.
Werbovetz, Karl
Lewis, Andrew
Johnsamuel, Jayasekar
description 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.
doi_str_mv 10.1016/j.bmcl.2005.09.001
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source MEDLINE; Access via ScienceDirect (Elsevier)
subjects 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
title Conformationally restricted analogs of Combretastatin A-4 derived from SU5416
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