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Sahabjada,
- Antiproliferative and Antibacterial Activity of Some Para-Substituted Benzylideneacetophenones and Establishing their Structure Activity Relationship
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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
References
- http://www.searo.who.int/india/topics/cancer/Cancer_resource_Commision_on_Macroeconomic_and_Health_Bg_P2_Cancers_current_scenario.pdf?ua=1
- http://www.worldcancerday.org/sites/wcd/files/private/130128_Cancer_Backgrounder.pdf
- http://www.worldheartfoundation.org/fileadmin/user_upload/documents/advocacy/resources/articles_series_report/WEF_havard_HE_globaleconomicburdennoncommunicabledisease_2011.pdf
- Chowrasia, D., Karthikeyan, C., Choure L., Sahabjada, Gupta, G. and Arshad, M., Synthesis, characterization and anti cancer activity of some fluorinated 3,6-diaryl-[1,2,4]triazolo[3,4-b][1,3,4] thiadiazoles. Arab. J. Chem., 2013 (in press).
- Chowrasia, D., Sharma, N., Chaurasia, A., Bharti, A. and Pratap, A., Chalcone as a principle pharmacophore for design and development of novel anticancer agents. Pharmacophore, 2016, 7(5), 35–42.
- Chowrasia, D., Sharma, N. and Arshad, M., In vitro antiproliferative activity of M. Azedarach; Pharma. Tut. Magz., 2017, 5(02), 46–49.
- Nascimento, G. G. F., Locatelli, J., Freitas, P. C. and Silva, G. L., Antibacterial activity of plant extracts and phytochemicals on antibiotic resistant bacteria. Braz. J. Microbiol., 2000, 31(4), 247–256.
- Mijovie, G., Andric, B., Terzic, D., Lopicic, M. and Dupanovic, B., Antibiotic susceptibility of Salmonella spp.: a comparison of two surveys with a 5 years interval. J. IMAB – Annu. Proc., (Scientific Papers). 2012, 18(1), 216–219.
- Bauer, A. W., Kirby, W. M., Sherris, J. C. and Turck, M., Antibiotic susceptibility testing by a standardized single disk method. Am. J. Clin. Pathol., 1966, 45(4), 493–496.
- Bhavnani, S. M. and Ballow, C. H., New agents for Gram-positive bacteria. Curr. Opin. Microbiol., 2000, 3(5), 528–534.
- WHO, ‘The Evolving Threat of Antimicrobial Resistance: Options for Action’, WHO Library Cataloguing-in-Publication Data, 2012.
- Wu, J. Z., Cheng, C. C., Shen, L. L., Wang, Z. K., Wu, S. B. and Li, W. L., Synthetic chalcones with potent antioxidant ability on H2O2-induced apoptosis in PC12 cells. Int. J. Mol. Sci., 2014, 15(10), 18525–18539.
- Kumar, C. S. C., Loh, W. S., Ooi, C. W., Quah, C. K. and Fun, H. K., Heteroarylchalcones: design, synthesis, X-ray crystal structures and biological evaluation. Molecules, 2013, 18(10), 12707–12724.
- Nguyen, T. T. N., Do, T. H., Huynh, T. N. P., Tran, C. D. T. and Thai, K. M., Synthesis and antibacterial activity of some heterocyclic chalcone analogues alone and in combination with antibiotics. Molecules, 2012, 17(6), 6684–6696.
- Hassan, S. Y., Synthesis, antibacterial and antifungal activity of some new pyrazoline and pyrazole derivatives. Molecules, 2013, 18(3), 2683–2711.
- Kang, J. E., Cho, J. K., Curtis-Long, M. J., Ryu, H. W., Kim, J. H. and Kim, H. J., Preparation of substituted pyridines and pyridazines with angiogenesis inhibiting activity for pharmaceutical use as antitumor agents. Molecules, 2013, 140–153.
- Solomon, V. R. and Lee, H., Anti-breast cancer activity of heteroarylchalcone derivatives. Biomed. Pharmacother., 2012, 66(3), 213–220.
- Kumar, D., Kumar, N. M., Akamatsu, K., Kusaka, E., Harada, H. and Ito, T., Synthesis and biological evaluation of indolylchalcones as antitumor agents. Bioorg. Med. Chem. Lett., 2010, 20(13), 3916–3919.
- Domyngueza, J. N., Charris, J. E., Loboa, G., De Domýnguezb, N. G., Moreno, M. M. and Riggione, F., Synthesis of quinolinylchalcones and evaluation of their antimalarial activity. Eur. J. Med. Chem., 2001, 36(6), 555–560.
- Hayat, F., Moseley, E., Salahuddin, A., Zyl, R. L. V. and Azam, A., Antiprotozoal activity of chloro-quinoline based chalcones. Eur. J. Med. Chem., 2011, 46(5), 1897–1905.
- Kotra, V., Ganapathy, S. and Adapa, S. R., Synthesis of new quinolinylchalcones as anticancer and anti-inflammatory agents. Indian J. Chem., 2010, 49(B), 1109–1116.
- Rizvi, S. U. F., Siddiqui, H. L., Johns, M., Detorio, M. and Schinazi, R. F., Anti-HIV-1 and cytotoxicity studies of piperidylthienylchalcones and their 2-pyrazoline derivatives. Med. Chem. Res., 2012, 21(11), 3741–3749.
- Ahmad, M. S., Sahabjada, Jafri, A., Ahmad, S., Afzal, M. and Arshad, M., Induction of apoptosis and antiproliferative activity of naringenin in human epidermoid carcinoma cell through ROS generation and cell cyle arrest. PLoS ONE, 2014, 9(10), e110003; doi:10.1371/journal.pone.0098409.
- Kaleem, S., Siddiqui, S., Hussain, A., Arshad, M., Akhtar, J., Rizvi, A. and Siddiqui, H. H., Eupalitin induces apoptosis in prostate carcinoma cells through ROS generation and increase of caspase3 activity. Cell Biol. Intern., 2016, 40(2), 196–203.