Copyright (c) 2022 AJC
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Design, Synthesis, Molecular Docking Studies and Biological Evaluation of Indole Fused Novel Pyrazole Derivatives
Corresponding Author(s) : N. Prasanna Lakshmi
Asian Journal of Chemistry,
Vol. 34 No. 6 (2022): Vol 34 Issue 6
Abstract
The present work deals with the sequence of indole fused novel pyrazole compounds (5a-l) synthesized by conventional method and were screened for anthelmintic, anticancer activities and molecular docking studies. All the newly synthesized compounds were characterized by IR, 1H NMR and Mass spectral analysis. Further, all the pyrazole derivatives were screened for anthelmintic activity using albendazole as standard drug and anticancer activity against MCF-7 and SKVO3 cell lines by MTT assay method. The results showed that compounds 5b and 5j exhibited good anticancer activity and compounds 5c, 5f, 5h and 5l exhibited potential anthelmintic activity. Additionally, the molecular docking studies of novel pyrazole derivatives were carried out to explain putative bonding interaction between the active site of EGFR enzyme and potent inhibitors.
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References
W.A. Ali, W.A. Wani, A. Khan, A. Haque, A. Ahmad, K. Saleem and N. Manzoor, Microb. Pathog., 53, 66 (2012); https://doi.org/10.1016/j.micpath.2012.04.005
R.V. Ragavan, V. Vijayakumar and N.S. Kumari, Eur. J. Med. Chem., 45, 1173 (2010); https://doi.org/10.1016/j.ejmech.2009.12.042
N.C. Desai, A.H. Makwana and K.M. Rajpara, J. Saudi Chem. Soc., 20, S334 (2016); https://doi.org/10.1016/j.jscs.2012.12.004
I. Ali, M.N. Lone, Z.A. Al-Othman, A. Al-Warthan and M.M. Sanagi, Curr. Drug Targets, 16, 711 (2015); https://doi.org/10.2174/1389450116666150309115922
B. Tiperciuc, V. Zaharia, I. Colosi, C. Moldovan, O. Crisan, A. Pirnau, L. Vlase, M. Duma and O. Oniga, J. Heterocycl. Chem., 49, 1407 (2012); https://doi.org/10.1002/jhet.1060
N. Kerru, L. Gummidi, S. Maddila, K.K. Gangu and S.B. Jonnalagadda, Molecules, 25, 1909 (2020); https://doi.org/10.3390/molecules25081909
C.D. Pawar, A.P. Sarkate, K.S. Karnik, S.S. Bahekar, D.N. Pansare, R.N. Shelke, C.S. Jawale and D.B. Shinde, Bioorg. Med. Chem. Lett., 26, 3525 (2016); https://doi.org/10.1016/j.bmcl.2016.06.030
G. Chen, Y. Wang, X. Hao, S. Mu and Q. Sun, Chem. Cent. J., 5, 37 (2011); https://doi.org/10.1186/1752-153X-5-37
K.R. Ethiraj, P. Nithya, V. Krishnakumar, A.J. Mathew and F.N. Khan, Res. Chem. Intermed., 39, 1833 (2012); https://doi.org/10.1007/s11164-012-0718-3
O. Abdel Hafez, K. Ahmed and E. Haggag, Molecules, 6, 396 (2011); https://doi.org/10.3390/60400396
R.F. Costa, L.C. Turones, K.V.N. Cavalcante, I.A. Rosa Jr., C.H. Xavier, L.P. Rosseto, H.B. Napolitano, P.F. da Silva Castro, M.L.F. Neto, G.M. Galvão, R. Menegatti, G.R. Pedrino, E.A. Costa, J.L.R Martins and J.O. Fajemiroye, Front. Pharmacol., 12, 666725 (2021); https://doi.org/10.3389/fphar.2021.666725
L. De la Cruz-Martínez, C. Duran-Becerra, M. González-Andrade, J.C. Páez-Franco, J.M. Germán-Acacio, J. Espinosa-Chávez, J.M. TorresValencia, J. Pérez-Villanueva, J.F. Palacios-Espinosa, O. Soria-Arteche and F. Cortés-Benítez, Molecules, 26, 4375 (2021); https://doi.org/10.3390/molecules26144375
J.J. Matilda and T.F.A. Fen Reji, Indian J. Chem.,60B, 1121 (2021).
M. Himaja, B. Sirisha, D. Moonjit and D. Munirasekhar, J. Indian Chem. Soc., 92, 908 (2015).
A. Venkanna, B. Siva, B. Poornima, P.R. Rao Vadaparthi, K.R. Prasad, K.A. Reddy, G.B.P. Reddy and K.S. Babu, Fitoterapia, 95, 102 (2014); https://doi.org/10.1016/j.fitote.2014.03.003
K.P. Leena, M.Z. Subin and C.H. Deepthy, Asian J. Pharm. Clin. Res., 10, 50 (2017).
X.Y. Meng, H.X. Zhang, M. Mezei and M. Cui, Curr. Computer-Aided Drug Design, 17, 146 (2014); https://doi.org/10.2174/157340911795677602