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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Beschreibung
Zusammenfassung:	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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm058046w