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 |
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container_title | Bioorganic & medicinal chemistry letters |
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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 |
format | Article |
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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.</description><subject>Animals</subject><subject>Antineoplastic agents</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Brain - cytology</subject><subject>Brain - drug effects</subject><subject>Brain - metabolism</subject><subject>Cell Division - drug effects</subject><subject>General aspects</subject><subject>Indoles - chemistry</subject><subject>Medical sciences</subject><subject>Models, Molecular</subject><subject>Molecular Conformation</subject><subject>Pharmacology. 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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.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>16213720</pmid><doi>10.1016/j.bmcl.2005.09.001</doi><tpages>4</tpages></addata></record> |
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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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