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Medicinal Chemistry


ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Design, Synthesis and Multidrug Resistance Reversal Activity Evaluation of 8-Oxocoptisine Derivatives

Author(s): Jian Bo Wu, Fan Lei, Xiang Juan Cui, Yun He, Li Hai, Juan Zhang and Yong Wu

Volume 8 , Issue 4 , 2012

Page: [742 - 748] Pages: 7

DOI: 10.2174/157340612801216148

Price: $65


Fifteen derivatives of 8-oxocoptisine were prepared based on that 8-oxocoptisine showed potent reversing effect against human cancer cells charactering multidrug resistance (MDR). The derivatives were evaluated for their growth inhibition and effects on reversing P-gp-mediated MDR against MCF-7/AMD cells. 12, 13-dinitro-8-oxocoptisine (6c), the most potential candidate with weak growth inhibition, significantly increased the sensitivity of adriamycin (ADM) against MCF-7/ADM cells by 213-fold at 10μM that was comparable to the reference compound verapamil. The preliminary structure-activity relationships (SARs) of these derivatives were discussed on the basis of the in vitro MDR reversal activities.

Keywords: Anti-cancer, MCF-7/AMD, multidrug resistance (MDR), 8-oxocoptisine, P-glycoprotein (P-gp), verapamil, MDR, Fumaria indica, breast cancer, chemotherapeutic agents

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