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
Abstract
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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