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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Chemical Characterization of N10-Substituted Acridones as Reversers of Multidrug Resistance in Cancer Cells

Author(s): Y.C. Mayur, Manjunath Gouda, Vadiraj S. Gopinath, S.M. Shanta Kumar and V.V.S. Rajendra Prasad

Volume 4, Issue 5, 2007

Page: [327 - 335] Pages: 9

DOI: 10.2174/157018007780867834

Price: $65

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)


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