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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(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’.
Keywords
Antiproliferative, Antibacterial Assay, Benzylideneacetophenone, MTT Assay.
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