双羟甲基取代的笼状二聚体1,4 - 二氢吡啶作为癌细胞中一类新型P - 糖蛋白调节剂的生物学评价
Biological evaluation of bishydroxymethyl-substituted cage dimeric 1,4-dihydropyridines as a novel class of p-glycoprotein modulating agents in cancer cells.
作者信息
Richter Martin, Molnár Jósef, Hilgeroth Andreas
机构信息
Institute of Pharmaceutical Chemistry, Martin-Luther-University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, 06120 Halle, Germany.
出版信息
J Med Chem. 2006 May 4;49(9):2838-40. doi: 10.1021/jm058046w.
PMID:16640345
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.
摘要
一系列N-取代的笼状二聚体1,4-二氢吡啶3a-e被评估为多药耐药（mdr）癌细胞中膜外排泵P-糖蛋白（P-gp）的抑制剂。讨论了构效关系（SAR）和细胞毒性特性。在与P-gp底物表柔比星的竞争研究中已证明了克服mdr的有效浓度。
Zotero 插件