S Desbene, H D Van, S Michel, F Tillequin, M Koch, F Schmidt, J C Florent, C Monneret, R Straub, J Czech, M Gerken, K Bosslet
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引用次数: 0
摘要
合成了由β - d -葡萄糖醛酸通过自燃间隔剂与耐多药逆转剂(维拉帕米、奎宁或双嘧达莫)连接而成的新型前药。其中四种因其降低细胞毒性和β -葡萄糖醛酸酶高效水解而被选中。将这些前药与β -d -葡醛酸间隔剂-阿霉素(HMR1826)联合使用，可在体外恢复耐多药菌株的敏感性。
Application of the ADEPT strategy to the MDR resistance in cancer chemotherapy.
New prodrugs consisting of a beta-D-glucuronic acid linked to a MDR reversal agent (verapamil, quinine or dipyridamole) through a self-immolative spacer were synthesized. Four of them were selected for their reduced cytoxicity and beta-glucuronidase enzymatic efficient hydrolysis. Combined use of these prodrugs with a beta-D-glucuronyl-spacer-doxorubicin (HMR1826) according to an ADEPT strategy restored in vitro the sensibility of a MDR resistant strain.
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