Singh Palwinder, Paul Kamaldeep
Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
Bioorg Med Chem. 2006 Nov 1;14(21):7183-6. doi: 10.1016/j.bmc.2006.06.060. Epub 2006 Jul 14.
The hybrid molecules having structural features of anticancer drug, 5-fluorouracil, and MDR modulator, propafenone, have been studied for their interactions with P-glycoprotein (P-gp). Some of the molecules (5, 8, and 9) show considerable interactions with P-gp and could be the potential candidates for their in vivo evaluation as MDR modulators. Further investigations show the dependence of P-gp interacting properties of these compounds on their physico-chemical parameters like logP and total polar surface area.
具有抗癌药物5-氟尿嘧啶和多药耐药性（MDR）调节剂普罗帕酮结构特征的杂合分子，已针对它们与P-糖蛋白（P-gp）的相互作用进行了研究。其中一些分子（5、8和9）与P-gp表现出显著的相互作用，有可能作为MDR调节剂进行体内评估。进一步的研究表明，这些化合物与P-gp相互作用的性质取决于它们的物理化学参数，如脂水分配系数（logP）和总极性表面积。
