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 designed to explore anti-cancer activity of novel bis-chalcones incorporating 1,3-diphenyl-1H-pyrazol 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 1,3-diphenyl-1H-pyrazol moiety as in vitro and in silico studies. Materials and Methods: condensation reactions, MTT Assay, Anticancer activity, Gene expression, DNA Fragmentation, DNA Damage and Molecular Docking study. 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 it a promising active component with further studies).
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.