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Anticancer Activities of Piperazine Ringed Chalcone Compounds and In Silico Studies

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Abstract

A new series of (E)-3-(substituted phenyl-1-(4-(piperazin-1-yl)phenyl)prop-2-en-1-one derivatives (I–XII) aiming to develop effective anticancer agents were synthesized. The anticancer activities of compound (I–XII) at 100, 50, 25 and 5 µM concentrations were investigated against HeLa (Human cervical cancer cells) and PC3 (Human prostate cancer cells) cancer cells by the BrdU ELISA assay. The anticancer activity results were compared with the standard compound 5-fluorouracil (5-FU). All molecules (except compound (II) for HeLa cancer cells and except compound (X) for the PC3 cell line) were found to be more active than 5-FU. Compound (XI) ((E)-1-(4-(piperazin-1-yl)phenyl)-3-(3-(trifluoromethoxy)phenyl)prop-2-en-1-one) showed high activity in both HeLa and PC3 cell lines, making it an ideal molecule candidate for binary interaction. Drug-likeness, pharmacokinetic properties, and physicochemical properties of all compounds (I–XII) were determined using SwissADME program.

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ACKNOWLEDGMENTS

The author thanks to Prof. Dr. Ayse Sahin Yaglioglu for her help in the construction and interpretation of anticancer tests.

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This work was supported by regular institutional funding, and no additional grants were obtained.

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  1. Department of Hair Care and Beauty Services, Yeşilyurt Vocational School, Malatya Turgut Özal University, 44210, Malatya, Turkey

    Bedriye Seda Kurşun Aktar

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Abbreviations: HeLa, human cervical cancer cells; PC3, human prostate cancer cells; 5-FU, 5-fluorouracil; NMR, nuclear magnetic resonance; FTIR, fourier transformed infrared spectroscopy; TLC, thin-layer chromatography; MgSO4, magnesıum sulfate; TPSA, topological polar surface area.

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Aktar, B.S.K. Anticancer Activities of Piperazine Ringed Chalcone Compounds and In Silico Studies. Russ J Bioorg Chem 49, 1023–1033 (2023). https://doi.org/10.1134/S1068162023050096

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