Synthesis, Antiproliferative Activity and In Silico Studies of Chalcones Derived From 4-(Imidazole-1-yl)Acetophenone

Year 2023, Volume: 10 Issue: 3, 861 - 868, 30.08.2023

Bedriye Seda Kurşun Aktar , Abdulraheem Mustafa Alkarabash , Ayşe Şahin Yağlıoğlu , Emine Elçin Oruç-emre

https://doi.org/10.18596/jotcsa.1313595

Abstract

In this study, the synthesis of chalcone compounds (1-11) derived from 4-(imidazol-1-yl)acetophenone and the structure determination of these compounds by various spectroscopic methods were carried out. The anticancer activities of compounds 1-11 were examined against HeLa and PC-3 cancer cells at four different concentrations (100, 50, 25, and 5 µM) using the BrdU ELISA assay. It was determined that all molecules except compounds 1 and 6 in HeLa cancer cells and compounds 2 and 8 against PC-3 cancer cells were more active against HeLa and PC-3 than the standard drug 5-fluorouracil (5-FU). The best activity against PC-3 cancer cells was compound 4 (IC50: 1.39±0.00 µM). In addition, compound 11 (IC50: 1.58±0.01 µM) was found to have the highest activity against HeLa cancer cells. Compound 4 against PC-3 cancer cell and compound 11 against HeLa cancer cell displayed cell selective activity. The ADME properties and drug similarities of the molecules 1-11 using the SwissADME software were investigated. According to these properties, compounds 1-11 were found to obey Lipinski rules.

Keywords

ADME, antiproliferative activity, HeLa cell line, in silico., PC-3 cell line

Supporting Institution

Amasya University Scientific Research Projects Governing Unit (BAPYB)

Project Number

FMB-BAP 22-0551

Thanks

This work was supported by Amasya University Scientific Research Projects Governing Unit (BAPYB) (Grant no: FMB-BAP 22-0551, Amasya, Turkey).

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