In:
Letters in Drug Design & Discovery, Bentham Science Publishers Ltd., Vol. 19, No. 11 ( 2022-11), p. 1007-1021
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.
Type of Medium:
Online Resource
ISSN:
1570-1808
DOI:
10.2174/1570180819666220301151631
Language:
English
Publisher:
Bentham Science Publishers Ltd.
Publication Date:
2022
SSG:
15,3
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