Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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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, V.V.S. Rajendra Prasad.

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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Article Details

VOLUME: 4
ISSUE: 5
Year: 2007
Page: [327 - 335]
Pages: 9
DOI: 10.2174/157018007780867834
Price: $58