Abstract
Synthesis of different N10-substituted-4-methyl acridones are described. The compounds are prepared with varying alkyl side chain length with propyl and butyl substitution and a tertiary amine group at the terminal end of the alkyl side chain. The structural requirement of in-vitro anti-cancer and reversal of drug resistance are studied. These compounds have been tested against the breast cancer cell lines MCF-7 and MCF- 7/Adr. The results show that compound 17 with four carbon spacer exhibited promising in-vitro anti-cancer and reversal of drug resistance in comparison to the other analogues. The studies show that the reversal of drug resistance is by P-gp inhibition.
Keywords: Acridones, Anti-cancer, P-glycoprotein (P-gp), Multidrug resistance (MDR)
Letters in Drug Design & Discovery
Title: Synthesis and Chemical Characterization of N10-Substituted Acridones as Reversers of Multidrug Resistance in Cancer Cells
Volume: 4 Issue: 5
Author(s): Y.C. Mayur, Manjunath Gouda, Vadiraj S. Gopinath, S.M. Shanta Kumar and V.V.S. Rajendra Prasad
Affiliation:
Keywords: Acridones, Anti-cancer, P-glycoprotein (P-gp), Multidrug resistance (MDR)
Abstract: Synthesis of different N10-substituted-4-methyl acridones are described. The compounds are prepared with varying alkyl side chain length with propyl and butyl substitution and a tertiary amine group at the terminal end of the alkyl side chain. The structural requirement of in-vitro anti-cancer and reversal of drug resistance are studied. These compounds have been tested against the breast cancer cell lines MCF-7 and MCF- 7/Adr. The results show that compound 17 with four carbon spacer exhibited promising in-vitro anti-cancer and reversal of drug resistance in comparison to the other analogues. The studies show that the reversal of drug resistance is by P-gp inhibition.
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Cite this article as:
Mayur Y.C., Gouda Manjunath, Gopinath S. Vadiraj, Shanta Kumar S.M. and Rajendra Prasad V.V.S., Synthesis and Chemical Characterization of N10-Substituted Acridones as Reversers of Multidrug Resistance in Cancer Cells, Letters in Drug Design & Discovery 2007; 4 (5) . https://dx.doi.org/10.2174/157018007780867834
DOI https://dx.doi.org/10.2174/157018007780867834 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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