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


Affiliations
1 University Institute of Pharmacy, Chhatrapati Shahu Ji Maharaj University, Kanpur 208 024, India
2 Department of Zoology, Lucknow University, Lucknow 226 007, India
 

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

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Authors

Deepak Chowrasia
University Institute of Pharmacy, Chhatrapati Shahu Ji Maharaj University, Kanpur 208 024, India
Nisha Sharma
University Institute of Pharmacy, Chhatrapati Shahu Ji Maharaj University, Kanpur 208 024, India
Ajay Kumar
University Institute of Pharmacy, Chhatrapati Shahu Ji Maharaj University, Kanpur 208 024, India
Vinod Dohrey
University Institute of Pharmacy, Chhatrapati Shahu Ji Maharaj University, Kanpur 208 024, India
Md. Arshad
Department of Zoology, Lucknow University, Lucknow 226 007, India
Asif Jafri
Department of Zoology, Lucknow University, Lucknow 226 007, India
Juhi Rais
Department of Zoology, Lucknow University, Lucknow 226 007, India
Madhu Gupta
Department of Zoology, Lucknow University, Lucknow 226 007, India
Sahabjada
Department of Zoology, Lucknow University, Lucknow 226 007, India

Abstract


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.

References





DOI: https://doi.org/10.18520/cs%2Fv114%2Fi02%2F391-396