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QSAR Studies On Substituted Bis- (Acridine-4-Carboxamides) As Potent DNA Intercalators

Author(s): S.V Sharma, L Venkateshwarlu, B Suresh

A series of bis-(acridine-4-carboxamide) analogues possessing significant cytotoxicity against P388 leukemia cell cultures, which were designed as bis-DNA intercalating agents, was subjected to the quantitative structure activity relationship analysis. Quantitative structure activity relationship studies by Fujita-Ban model gave excellent correlations (correlation coefficient, r=0.997) for the 24 compounds included in the final regression analysis. It was observed that substitutions on position 5 favor the activity while any group on position 6 decreases the activity strongly. Theseresults will be useful in designing 'lead' compounds to be useful as bis-DNA intercalators for the therapy of leukemia.