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Letters in Drug Design & Discovery

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ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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Research Article

Synthesis and Anticancer Activities of Novel Bis-chalcones Incorporating the 1,3-diphenyl-1H-pyrazole Moiety: In Silico and In Vitro Studies

Author(s): Magda F. Mohamed, Farid M. Sroor*, Shahinda E. Elsayed, Karima F. Mahrous, Lamiaa Mageed, Mahmoud Khaled Hanafy, Sherif A. Ibrahim, Ahmed H. M. Elwahy* and Ismail A. Abdelhamid*

Volume 19, Issue 11, 2022

Published on: 12 May, 2022

Page: [1007 - 1021] Pages: 15

DOI: 10.2174/1570180819666220301151631

Price: $65

Abstract

A new series of bis-chalcones 5-10 has been prepared by the condensation reaction of one equivalent of bis(acetophenones) 3a-f with two equivalents of 1,3-diphenyl-1H-pyrazole-4-carbaldehyde 4. The newly prepared compounds 5-10 have been fully characterized and evaluated as in vitro anticancer agents against a panel of human cancer cell lines A431, A549, PC3, and a normal human skin fibroblast BJ1.

Aims: The current work is designed to explore the anti-cancer activity of novel bis-chalcones incorporating a 1,3-diphenyl-1H-pyrazole moiety.

Background: Chalcones represent one of the most important organic compounds that have been attracting the interest of many researchers in drug discovery.

Objective: The present study was carried out to explore anti-cancer activity of novel bis-chalcones incorporating a 1,3-diphenyl-1H-pyrazole moiety as in vitro and in silico studies.

Materials and Methods: We used the condensation reaction to prepare bis-chalcones incorporating 1,3- diphenyl-1H-pyrazole moiety. The MTT Assay, Anti-cancer activity, Gene expression, DNA Fragmentation, DNA Damage, and Molecular docking were investigated.

Results: Compounds 5 and 9 were found to be the most promising compounds in the prepared series with IC50 (50.3 and 50.1 μg/ml, respectively) against epidermoid cancer cell line A431 compared to doxorubicin as a reference drug.

Conclusion: All of these results showed that chalcones 5 and 9 have promising anti-cancer properties without cytotoxic effect, which could make them a promising active component for further studies.

Keywords: Chalcones, anti-cancer, DNA damage, DNA fragmentation, gene expression, molecular docking study.

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