Antiproliferative and Antibacterial Activity of Some Para-Substituted Benzylideneacetophenones and Establishing their Structure Activity Relationship

We report here in-vitro antiproliferative and antibacterial activity of para -substituted benzylideneacetophenones and established their structure activity relationship to optimize para position as a biologically-oriented-synthetic target for design of small moleculebased future anticancer/antibacterial agents. Among synthesized compounds, 1c exhibits excellent antiproliferative activity against human osteosarcoma cell line (MG-63) compared to 1b and 1a suggesting dimethylamino (–N(CH 3 ) 2 ) functionality as a better para -substituted analogue for in-future anticancer agents. Similarly antibacterial screening of the aforesaid compounds against different strains of Gramnegative and Gram-positive bacteria reveals methoxy (–OCH 3 ) rather than dimethylamino (–N(CH 3 ) 2 ) as a better para -substituted functionality on ring B comparatively. From our results, we justify our theory ‘lipophilicity affects antibacterial activity’.