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Jafri, Asif
- Antiproliferative and Antibacterial Activity of Some Para-Substituted Benzylideneacetophenones and Establishing their Structure Activity Relationship
Abstract Views :263 |
PDF Views:74
Authors
Deepak Chowrasia
1,
Nisha Sharma
1,
Ajay Kumar
1,
Vinod Dohrey
1,
Md. Arshad
2,
Asif Jafri
2,
Juhi Rais
2,
Madhu Gupta
2,
Sahabjada
2
Affiliations
1 University Institute of Pharmacy, Chhatrapati Shahu Ji Maharaj University, Kanpur 208 024, IN
2 Department of Zoology, Lucknow University, Lucknow 226 007, IN
1 University Institute of Pharmacy, Chhatrapati Shahu Ji Maharaj University, Kanpur 208 024, IN
2 Department of Zoology, Lucknow University, Lucknow 226 007, IN
Source
Current Science, Vol 114, No 02 (2018), Pagination: 391-396Abstract
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.Full Text
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- Synthetic Modulation Including Structure Establishment, Antiproliferative Activity of Some p-Aryl Substituted (Z)-2-Cyanoethylideneacetohydrazides, and their Structure Activity Relationship
Abstract Views :228 |
PDF Views:79
Authors
Deepak Chowrasia
1,
Nisha Sharma
1,
Ajay Kumar
1,
Md Arshad
2,
Sahabjada Siddiqui
2,
Asif Jafri
2,
Juhi Rahis
2
Affiliations
1 University Institute of Pharmacy, Chhatrapati Shahu ji Maharaj (CSJM) University, Kalyanpur, Kanpur 208 024, IN
2 Department of Zoology, Lucknow University, Lucknow 226 007, IN
1 University Institute of Pharmacy, Chhatrapati Shahu ji Maharaj (CSJM) University, Kalyanpur, Kanpur 208 024, IN
2 Department of Zoology, Lucknow University, Lucknow 226 007, IN
Source
Current Science, Vol 115, No 12 (2018), Pagination: 2287-2290Abstract
A series of p-substituted aryl-2-cyanoethylideneacetohydrazides derivatives (2a-j) were successfully synthesized in the laboratory (yield 60–80%). The synthesized compounds were screened for their antiproliferative activity against MCF-7 (estrogen dependent human breast cancer cell line), SaOS-2 (osteosarcoma cell line), and K562 (myeloid leukemia cell line) by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide) reduction assay. They showed moderate to mild antiproliferative activity, (2j) being the most potent in the series with an IC50 55, 64 and 35 μM against MCF-7, SaOS-2 and K562 cell lines, depict p-nitro as a better antiproliferative substituent comparatively. We have also tested the hypothesis – ‘Electron withdrawing phenomenon affects antiproliferative activity’.Keywords
Cancer, Cyanoacetohydrazide, Electron Withdrawing Ring Substituent, MTT Assay.Full Text
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