Antiproliferative and antibacterial activity of some para-substituted benzylideneacetophenones and establishing their structure activity relationship

摘要

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(CH3)(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 (-OCH3) rather than dimethylamino (-N(CH3)(2)) as a better para-substituted functionality on ring B comparatively. From our results, we justify our theory 'lipophilicity affects antibacterial activity'.