Comparative Study on the MDR Reversal Effects of Selected ChalconesReport as inadecuate

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International Journal of Medicinal ChemistryVolume 2011 2011, Article ID 530780, 7 pages

Research Article

Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Acad. G. Bonchev Street Bl. 9, Sofia 1113, Bulgaria

Department of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, 10 Dóm tér, 6720 Szeged, Hungary

Received 30 September 2010; Revised 30 November 2010; Accepted 22 December 2010

Academic Editor: Benedetto Natalini

Copyright © 2011 A. B. Ivanova et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


Based on the structure of three previously established lead compounds, fifteen selected chalcones were synthesized and evaluated for their multidrug resistance MDR reversal activity on mouse lymphoma cells. The most active chalcones were stronger revertants than the positive control, verapamil. In the model of combination chemotherapy, the interactions between the anticancer drug doxorubicin and two of the most effective compounds were measured in vitro, on human MDR1 gene transfected mouse lymphoma cells, showing that the type of interaction for one of these compounds was indifferent while that for the other one was additive. Furthermore, two chalcones inhibited 50% of cell proliferation in concentration of around 0.4 μg-mL and were from 2- to 100-fold more active than the most chalcones. The structure-activity relationships were obtained and discussed in view of their usefulness for the design of chalcone-like P-gp modulators and drugs able to treat resistant cancers.

Author: A. B. Ivanova, D. I. Batovska, I. T. Todorova, B. A. Stamboliyska, J. Serly, and J. Molnar



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