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 |
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container_title | Bioorganic & medicinal chemistry letters |
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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 |
format | Article |
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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.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2013.04.078</identifier><identifier>PMID: 23790539</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>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</subject><ispartof>Bioorganic & medicinal chemistry letters, 2013-08, Vol.23 (15), p.4465-4468</ispartof><rights>2013 Elsevier Ltd</rights><rights>Copyright © 2013 Elsevier Ltd. 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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.</description><subject>Anti-microtubule agents</subject><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Bibenzyls - pharmacology</subject><subject>Breast cancer</subject><subject>Cell Line, Tumor</subject><subject>Cell Proliferation - drug effects</subject><subject>Drug Design</subject><subject>Humans</subject><subject>Polymerization - drug effects</subject><subject>Tubulin - chemistry</subject><subject>Tubulin - metabolism</subject><subject>Tubulin inhibitors</subject><subject>Tubulin Modulators - chemical synthesis</subject><subject>Tubulin Modulators - chemistry</subject><subject>Tubulin Modulators - pharmacology</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2013</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkDlPxDAQRi0EguX4AxQoJQUJ4yOHJRrEckkr0YBEZ_kYg1fZGOIEiX9PVguUUM0U73vFI-SYQkGBVufLwqxsWzCgvABRQN1skRkVlci5gHKbzEBWkDdSPO-R_ZSWAFSAELtkj_FaQsnljMznmMJLd5alz254nf6U6c5lJsQ2vgSr2ywNowuYsuizLn5gmw2jGdvQZaF7DSYMsU-HZMfrNuHR9z0gTzfXj1d3-eLh9v7qcpFb3sghRyeRlrX1lHlXM9sIr9Foa0XpTWMZQ1c3Brik0oE1tRbAtbelYYjMCM8PyOnG-9bH9xHToFYhWWxb3WEck6IlQF1WEuB_lDcUpGQVnVC2QW0fU-rRq7c-rHT_qSiodWi1VOvQah1agVBT6Gl08u0fzQrd7-Sn7ARcbACcgnwE7FWyATuLLvRoB-Vi-Mv_BbRvkAw</recordid><startdate>20130801</startdate><enddate>20130801</enddate><creator>Sun, Yanjun</creator><creator>Pandit, Bulbul</creator><creator>Chettiar, Somsundaram N.</creator><creator>Etter, Jonathan P.</creator><creator>Lewis, Andrew</creator><creator>Johnsamuel, Jayasekar</creator><creator>Li, Pui-Kai</creator><general>Elsevier Ltd</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20130801</creationdate><title>Design, synthesis and biological studies of novel tubulin inhibitors</title><author>Sun, Yanjun ; 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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.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>23790539</pmid><doi>10.1016/j.bmcl.2013.04.078</doi><tpages>4</tpages></addata></record> |
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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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