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   
Heidi S. Abd ElMonaem1, Naglaa I. Abdel-Aziz1 & 2, Mohammad A. Morsy2 & 3, Farid A. Badria4, Fardous ElSenduny5, Mahmoud B. El-Ashmawy1, Mohamed A. Moustafa1 & 6

1Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.

2Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Delta University for Science and Technology, Egypt.

3Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, Egypt.

4Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.

5Department of Biochemistry, Faculty of Science, Mansoura University, Mansoura 35516, Egypt.

6Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Kingdom of Saudi Arabia.

Open Access   

Published:  May 30, 2018

DOI: 10.7324/JAPS.2018.8510
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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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