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Medicinal Chemistry

Author(s): Y. C. Mayur, Osman Ahmad, V. V.S. Rajendra Prasad, M. N. Purohit, N. Srinivasulu and S. M. Shanta Kumar

DOI: 10.2174/157340608785700180

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Synthesis of 2-Methyl N10-Substituted Acridones as Selective Inhibitors of Multidrug Resistance (MDR) Associated Protein in Cancer Cells

Page: [457 - 465] Pages: 9

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Abstract

A series of N10-substituted-2-methyl acridone derivatives are synthesized and are examined for its ability to reverse P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in breast cancer cell lines MCF-7 and MCF-7/Adr. The structural requirement of in-vitro anti-cancer and reversal of drug resistance are studied. The results showed that compound 16 with four carbon spacer exhibited promising in-vitro anti-cancer and reversal of drug resistance in comparison to the other analogues.

Keywords: Acridones, anti-cancer, P-glycoprotein (P-gp), multidrug resistance (MDR)