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 mdr have been demonstrated in competition studies with the P-gp substrate epirubicin.
Richter
Martin
M
Institute of Pharmaceutical Chemistry, Martin-Luther-University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, 06120 Halle, Germany.
Molnár
Jósef
J
Hilgeroth
Andreas
A
D018435:ATP Binding Cassette Transporter, Subfamily B / Q000378:metabolism*; D000818:Animals; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004095:Dihydropyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D019281:Dimerization; D006900:Hydroxylation; D008745:Methylation; D051379:Mice; D015394:Molecular Structure; D009369:Neoplasms / Q000378:metabolism*; D013329:Structure-Activity Relationship
D018435:ATP Binding Cassette Transporter, Subfamily B; D004095:Dihydropyridines; C038806:1,4-dihydropyridine