Biological Evaluation of Bishydroxymethyl-Substituted Cage Dimeric 1,4-Dihydropyridines as a Novel Class of P-Glycoprotein Modulating Agents in Cancer Cells

A series of N-substituted cage dimeric 1,4-dihydropyridines 3a−e was evaluated as inhibitors of membrane efflux pump P-glycoprotein (P-gp) in multidrug resistant (mdr) cancer cells. Structure−activity relationships (SAR) and cytotoxic properties are discussed. Effective concentrations for overcoming...

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Veröffentlicht in:	Journal of medicinal chemistry 2006-05, Vol.49 (9), p.2838-2840
Hauptverfasser:	Richter, Martin, Molnár, Jósef, Hilgeroth, Andreas
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic agents ATP Binding Cassette Transporter, Sub-Family B - metabolism Biological and medical sciences Cell Line, Tumor Cell Proliferation - drug effects Dihydropyridines - chemical synthesis Dihydropyridines - chemistry Dihydropyridines - pharmacology Dihydropyridines - toxicity Dimerization General aspects Hydroxylation Medical sciences Methylation Mice Molecular Structure Neoplasms - metabolism Pharmacology. Drug treatments Structure-Activity Relationship
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container_title	Journal of medicinal chemistry
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creator	Richter, Martin Molnár, Jósef Hilgeroth, Andreas
description	A series of N-substituted cage dimeric 1,4-dihydropyridines 3a−e was evaluated as inhibitors of membrane efflux pump P-glycoprotein (P-gp) in multidrug resistant (mdr) cancer cells. Structure−activity relationships (SAR) and cytotoxic properties are discussed. Effective concentrations for overcoming mdr have been demonstrated in competition studies with the P-gp substrate epirubicin.
doi_str_mv	10.1021/jm058046w
format	Article
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Med. Chem</addtitle><description>A series of N-substituted cage dimeric 1,4-dihydropyridines 3a−e was evaluated as inhibitors of membrane efflux pump P-glycoprotein (P-gp) in multidrug resistant (mdr) cancer cells. Structure−activity relationships (SAR) and cytotoxic properties are discussed. 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Drug treatments</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Richter, Martin</creatorcontrib><creatorcontrib>Molnár, Jósef</creatorcontrib><creatorcontrib>Hilgeroth, Andreas</creatorcontrib><collection>Istex</collection><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>Journal of medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Richter, Martin</au><au>Molnár, Jósef</au><au>Hilgeroth, Andreas</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Biological Evaluation of Bishydroxymethyl-Substituted Cage Dimeric 1,4-Dihydropyridines as a Novel Class of P-Glycoprotein Modulating Agents in Cancer Cells</atitle><jtitle>Journal of medicinal chemistry</jtitle><addtitle>J. Med. Chem</addtitle><date>2006-05-04</date><risdate>2006</risdate><volume>49</volume><issue>9</issue><spage>2838</spage><epage>2840</epage><pages>2838-2840</pages><issn>0022-2623</issn><eissn>1520-4804</eissn><coden>JMCMAR</coden><abstract>A series of N-substituted cage dimeric 1,4-dihydropyridines 3a−e was evaluated as inhibitors of membrane efflux pump P-glycoprotein (P-gp) in multidrug resistant (mdr) cancer cells. Structure−activity relationships (SAR) and cytotoxic properties are discussed. Effective concentrations for overcoming mdr have been demonstrated in competition studies with the P-gp substrate epirubicin.</abstract><cop>Washington, DC</cop><pub>American Chemical Society</pub><pmid>16640345</pmid><doi>10.1021/jm058046w</doi><tpages>3</tpages></addata></record>
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subjects	Animals Antineoplastic agents ATP Binding Cassette Transporter, Sub-Family B - metabolism Biological and medical sciences Cell Line, Tumor Cell Proliferation - drug effects Dihydropyridines - chemical synthesis Dihydropyridines - chemistry Dihydropyridines - pharmacology Dihydropyridines - toxicity Dimerization General aspects Hydroxylation Medical sciences Methylation Mice Molecular Structure Neoplasms - metabolism Pharmacology. Drug treatments Structure-Activity Relationship
title	Biological Evaluation of Bishydroxymethyl-Substituted Cage Dimeric 1,4-Dihydropyridines as a Novel Class of P-Glycoprotein Modulating Agents in Cancer Cells
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