新型N-酰氧基-1,4-二氢吡啶作为P-糖蛋白抑制剂的构效关系
Structure-activity relationships of novel N-acyloxy-1,4-dihydropyridines as P-glycoprotein inhibitors.
作者信息
Voigt Burkhardt, Coburger Claudius, Monár Joséf, Hilgeroth Andreas
机构信息
Institute of Pharmacy, Martin Luther University, Halle, Germany.
出版信息
Bioorg Med Chem. 2007 Aug 1;15(15):5110-3. doi: 10.1016/j.bmc.2007.05.036. Epub 2007 May 18.
PMID:17533131
Abstract
Series of novel N-acyloxy-1,4-dihydropyridines have been synthesized and evaluated as P-glycoprotein inhibitors in an in vitro assay to estimate their potential to act as multidrug resistance modulators in cancer cells. Structure-activity relationships are discussed and prove a significant and regiospecific influence of certain functional groups.
摘要
已合成了一系列新型的N-酰氧基-1,4-二氢吡啶，并在体外试验中作为P-糖蛋白抑制剂进行了评估，以估计它们在癌细胞中作为多药耐药调节剂的潜力。讨论了构效关系，并证明了某些官能团具有显著的区域特异性影响。
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