期刊
LETTERS IN DRUG DESIGN & DISCOVERY
卷 4, 期 5, 页码 327-335出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/157018007780867834
关键词
acridones; anti-cancer; P-glycoprotein (P-gp); multidrug resistance (MDR)
Synthesis of different N-10-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 MCF7/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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