Research Article | Volume: 8, Issue: 5, May, 2018

Synthesis, In Vitro Antiproliferative Evaluation and Molecular Docking of New tetrazole-chalcone and tetrazole-pyrazoline Hybrids

Heidi S. Abd ElMonaem Naglaa I. Abdel-Aziz Mohammad A. Morsy Farid A. Badria Fardous ElSenduny Mahmoud B. El-Ashmawy Mohamed A. Moustafa   

Open Access   

Published:  May 30, 2018

DOI: 10.7324/JAPS.2018.8510
Abstract

New hybrids of tetrazole moiety with different chalcone derivatives were synthesized. The reaction of these chalcones with hydrazine hydrate resulted in the formation of tetrazole-pyrazoline hybrids. Evaluation of the in vitro antiproliferative activity of all newly synthesized hybrids against three cancer cell lines and Vero-B normal cell line, using MTT-based assay, was performed. Most of the chalcone derivatives exerted superior activity against colon HCT- 116 and prostate PC-3 cell lines, in comparison with cisplatin (IC50 = 20 and 5 μg/ml) and 5-FU (IC50 = 17.3 and 21.4 μg/ml), respectively. Compound 5a was found to be the most active antiproliferative agent against colon HCT-116 and prostate PC-3 cell lines (IC50 = 0.6 and 1.6 μg/ml) with high selectivity indices (SI = 6.66 and 2.50), respectively. Compound 8f, in particular, displayed a wider spectrum of activity that included, in addition, excellent effect against breast MCF-7 cell lines with SI = 2.75. The available docking results revealed a good binding of 5b with HDAC2 and CYP17A1 that endorses the in vitro biological activity against the tested colon and prostate cell lines.


Keyword:     Tetrazole Chalcone Pyrazoline Antiproliferative Molecular docking.


Citation:

Abd ElMonaem HS, Abdel-Aziz NI, Morsy MA, Badria FA, ElSenduny F, El-Ashmawy MB, Moustafa MA. Synthesis, In Vitro Antiproliferative Evaluation and Molecular Docking of New tetrazole-chalcone and tetrazole-pyrazoline Hybrids. J App Pharm Sci, 2018; 8(05): 075-087.

Copyright: © The Author(s). This is an open-access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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