- Journal of the Turkish Chemical Society Section A: Chemistry
- Vol: 10 Issue: 3
- Synthesis, Antiproliferative Activity and In Silico Studies of Chalcones Derived From 4-(Imidazole-1...
Synthesis, Antiproliferative Activity and In Silico Studies of Chalcones Derived From 4-(Imidazole-1-yl)Acetophenone
Authors : Bedriye Seda Kurşun Aktar, Abdulraheem Mustafa Alkarabash, Ayşe Şahin Yağlioğlu, Emine Elçin Oruç-emre
Pages : 861-868
Doi:10.18596/jotcsa.1313595
View : 62 | Download : 72
Publication Date : 2023-08-30
Article Type : Research Article
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