Copyright (c) 2019 AJC
This work is licensed under a Creative Commons Attribution 4.0 International License.
Synthesis and Characterization of 2-Pyrazoline Derivatives and their in silico and in vitro Studies on Antimicrobial and Anticancer Activities
Corresponding Author(s) : M.R. Ezhilarasi
Asian Journal of Chemistry,
Vol. 31 No. 10 (2019): Vol 31 Issue 10
Abstract
The new series of 1-(4,5-dihydro-5-phenyl-3-diphenylpyrazol-1-yl)butan-1-one derivatives were synthesized by cyclization method using biphenyl chalcone with n-butyric acid and hydrazine hydrate. The synthesized 1-(4,5-dihydro-5-phenyl-3-diphenylpyrazol-1-yl)butan-1-one derivatives chemical structures were confirmed from spectral data such as FT-IR, 1H and 13C NMR. 2-Pyrazoline derivatives were docked with bacterial (1UAG) and breast cancer (1OQA) protein. Based on high binding affinity score, the best compound was subjected to in vitro anticancer activity by MTT assay. Also, antimicrobial activity were studied for synthesized 2-pyrazoline derivatives.
Keywords
Download Citation
Endnote/Zotero/Mendeley (RIS)BibTeX
- S.S. Abd El-Karim, M.M. Anwar, N.A. Mohamed, T. Nasr and S.A. Elseginy, Bioorg. Chem., 63, 1 (2015); https://doi.org/10.1016/j.bioorg.2015.08.006.
- Y.-C. Jung, S. Han, L. Hua, Y.-H. Ahn, H. Cho, C.-J. Lee, H. Lee, Y.-Y. Cho, J.-H. Ryu, R. Jeon and W.-Y. Kim, Biochem. Biophys. Res. Commun., 470, 294 (2016); https://doi.org/10.1016/j.bbrc.2016.01.066.
- A. Abdel-Aziz, H.S.A. El-Zahabi and K.M. Dawood, Eur. J. Med. Chem., 45, 2427 (2010); https://doi.org/10.1016/j.ejmech.2010.02.026.
- R. Dayam, F. Aiello, J. Deng, Y. Wu, A. Garofalo, X. Chen and N. Neamati, J. Med. Chem., 49, 4526 (2006); https://doi.org/10.1021/jm051296s.
- Y.R. Liu, J.-Z. Luo, P.-P. Duan, J. Shao, B.-X. Zhao and J.-Y. Miao, Bioorg. Med. Chem. Lett., 22, 6882 (2012); https://doi.org/10.1016/j.bmcl.2012.09.032.
- I. Vujasinovic, A. Paravic-Radièevic, K. Mlinaric-Majerski, K. Brajsa and B. Bertosa, Bioorg. Med. Chem., 20, 2101 (2012); https://doi.org/10.1016/j.bmc.2012.01.032.
- A.M. Farag, K.A.K. Ali, T.M.A. El-Debss, A.S. Mayhoub, A.-G.E. Amr, N.A. Abdel-Hafez and M.M. Abdulla, Eur. J. Med. Chem., 45, 5887 (2010); https://doi.org/10.1016/j.ejmech.2010.09.054.
- A.M. Farag, A.S. Mayhoub, T.M.A. Eldebss, A.-G.E. Amr, K.A.K. Ali, N.A. Abdel-Hafez and M.M. Abdulla, Arch. Pharm. Chem. Life Sci., 343, 384 (2010); https://doi.org/10.1002/ardp.200900176.
- H.A. Abdel-Aziz, A.A.I. Mekawey and K.M. Dawood, Eur. J. Chem., 44, 3637 (2009); https://doi.org/10.1016/j.ejmech.2009.02.020.
- R. Sridhar, P.T. Perumal, S. Etti, G. Shanmugam, M.N. Ponnuswamy, V.R. Prabavathy and N. Mathivanan, Bioorg. Med. Chem. Lett., 14, 6035 (2004); https://doi.org/10.1016/j.bmcl.2004.09.066.
- R. Chinnamanayakar, M.R. Ezhilarasi, B. Prabha and Kulandhaivel, Asian J. Chem., 30, 783 (2018); https://doi.org/10.14233/ajchem.2018.20992.
- R. Sri Dharani, R. Ranjitha, R. Sripathi, K.S. Ali Muhammad and S. Ravi, Asian J. Pharm. Clin. Res., 9, 121 (2016); https://doi.org/10.22159/ajpcr.2016.v9i5.12693.
- L.B. Talarico, R.G.M. Zibetti, P.C.S. Faria, L.A. Scolaro, M.E.R. Duarte, M.D. Noseda, C.A. Pujol and E.B. Damonte, Int. J. Biol. Macromol., 34, 63 (2004); https://doi.org/10.1016/j.ijbiomac.2004.03.002.
References
S.S. Abd El-Karim, M.M. Anwar, N.A. Mohamed, T. Nasr and S.A. Elseginy, Bioorg. Chem., 63, 1 (2015); https://doi.org/10.1016/j.bioorg.2015.08.006.
Y.-C. Jung, S. Han, L. Hua, Y.-H. Ahn, H. Cho, C.-J. Lee, H. Lee, Y.-Y. Cho, J.-H. Ryu, R. Jeon and W.-Y. Kim, Biochem. Biophys. Res. Commun., 470, 294 (2016); https://doi.org/10.1016/j.bbrc.2016.01.066.
A. Abdel-Aziz, H.S.A. El-Zahabi and K.M. Dawood, Eur. J. Med. Chem., 45, 2427 (2010); https://doi.org/10.1016/j.ejmech.2010.02.026.
R. Dayam, F. Aiello, J. Deng, Y. Wu, A. Garofalo, X. Chen and N. Neamati, J. Med. Chem., 49, 4526 (2006); https://doi.org/10.1021/jm051296s.
Y.R. Liu, J.-Z. Luo, P.-P. Duan, J. Shao, B.-X. Zhao and J.-Y. Miao, Bioorg. Med. Chem. Lett., 22, 6882 (2012); https://doi.org/10.1016/j.bmcl.2012.09.032.
I. Vujasinovic, A. Paravic-Radièevic, K. Mlinaric-Majerski, K. Brajsa and B. Bertosa, Bioorg. Med. Chem., 20, 2101 (2012); https://doi.org/10.1016/j.bmc.2012.01.032.
A.M. Farag, K.A.K. Ali, T.M.A. El-Debss, A.S. Mayhoub, A.-G.E. Amr, N.A. Abdel-Hafez and M.M. Abdulla, Eur. J. Med. Chem., 45, 5887 (2010); https://doi.org/10.1016/j.ejmech.2010.09.054.
A.M. Farag, A.S. Mayhoub, T.M.A. Eldebss, A.-G.E. Amr, K.A.K. Ali, N.A. Abdel-Hafez and M.M. Abdulla, Arch. Pharm. Chem. Life Sci., 343, 384 (2010); https://doi.org/10.1002/ardp.200900176.
H.A. Abdel-Aziz, A.A.I. Mekawey and K.M. Dawood, Eur. J. Chem., 44, 3637 (2009); https://doi.org/10.1016/j.ejmech.2009.02.020.
R. Sridhar, P.T. Perumal, S. Etti, G. Shanmugam, M.N. Ponnuswamy, V.R. Prabavathy and N. Mathivanan, Bioorg. Med. Chem. Lett., 14, 6035 (2004); https://doi.org/10.1016/j.bmcl.2004.09.066.
R. Chinnamanayakar, M.R. Ezhilarasi, B. Prabha and Kulandhaivel, Asian J. Chem., 30, 783 (2018); https://doi.org/10.14233/ajchem.2018.20992.
R. Sri Dharani, R. Ranjitha, R. Sripathi, K.S. Ali Muhammad and S. Ravi, Asian J. Pharm. Clin. Res., 9, 121 (2016); https://doi.org/10.22159/ajpcr.2016.v9i5.12693.
L.B. Talarico, R.G.M. Zibetti, P.C.S. Faria, L.A. Scolaro, M.E.R. Duarte, M.D. Noseda, C.A. Pujol and E.B. Damonte, Int. J. Biol. Macromol., 34, 63 (2004); https://doi.org/10.1016/j.ijbiomac.2004.03.002.