Design, synthesis, biological evaluation, molecular docking and QSAR studies of 2,4-dimethylacridones as anticancer agents

Multidrug resistance in cancer is an unmet challenge and drawback for the failure of many chemotherapeutic drugs. Search for targeted, effective drug with minimum toxicity is an urgent need. An attempt has been made to explore the chemosensitizing ability of 2,4-dimethylacridones with alkyl side chain containing substituting tertiary amines at the end of the side chain. Considering the structural features required for the MDR reversal activity, 2,4-dimethylacridone with propyl and butyl side chain containing various tertiary amino groups like morpholinyl, piperidinyl, N-methyl piperazinyl, N,N-diethylamino, N-diethanolamino, β-hydroxylethyl piperazino at the terminus of the alkyl side chain have been synthesized, characterized and screened for anticancer and MDR modulation activity.147