7-Diethylamino-3(2'-benzoxazolyl)-coumarin for multidrug resista
 

<dl class="AbstractPlusReport"><dt class="head">1: Biochem Pharmacol. 2009 Jun 15;77(12):1773-9. Epub 2009 Mar 19.http://www.ncbi.nlm.nih.gov/corehtml...PubMedLink.gif <script language="JavaScript1.2"><!-- var Menu19428332 = [ ["UseLocalConfig", "jsmenu3Config", "", ""], ["Substance (MeSH Keyword)" , "window.top.location='/sites/entrez?Db=pcsubstance&DbFrom=pubmed&Cmd=Link&LinkN ame=pubmed_pcsubstance_mesh&LinkReadableName=Subst ance%20(MeSH%20Keyword)&IdsFromResult=19428332&ord inalpos=1&itool=EntrezSystem2.PEntrez.Pubmed.Pubme d_ResultsPanel.Pubmed_DiscoveryPanel.Pubmed_RVAbst ractPlus' ", "", ""], ["LinkOut", "window.top.location='/sites/entrez?Cmd=ShowLinkOut&Db=pubmed&TermToSearch=1942 8332&ordinalpos=1&itool=EntrezSystem2.PEntrez.Pubm ed.Pubmed_ResultsPanel.Pubmed_DiscoveryPanel.Pubme d_RVAbstractPlus' ", "", ""] ] --></script>Links
</dt><dd class="abstract"> 7-Diethylamino-3(2'-benzoxazolyl)-coumarin is a novel microtubule inhibitor with antimitotic activity in multidrug resistant cancer cells.

<!--AuthorList-->Kim SN, Kim NH, Park YS, Kim H, Lee S, Wang Q, Kim YK.
KIST Gangneung Institute, Gangneung, Republic of Korea.
Microtubules are a proven target for anticancer drug development because they are critical for mitotic spindle formation and the separation of chromosomes at mitosis. We here report a novel synthetic microtubule inhibitor 7-diethylamino-3(2'-benzoxazolyl)-coumarin (DBC). DBC causes destabilization of microtubules, leading to a cell cycle arrest at G(2)/M stage. In addition, human cancer cells are more sensitive to DBC (IC(50) 44.8-475.2nM) than human normal fibroblast (IC(50) 7.9microM), and DBC induces apoptotic cell death of cancer cells. Furthermore, our data show that DBC is a poor substrate of drug efflux pumps and effective against multidrug resistant (MDR) cancer cells. Taken together, these results describe a novel pharmacological property of DBC as a microtubule inhibitor, which may make it an attractive new agent for treatment of MDR cancer.
PMID: 19428332 [PubMed - indexed for MEDLINE]
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