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 ŞAHİN YAĞLIOĞLU, Emine Elçin ORUÇ-EMRE

Pages : 861-868

Doi:10.18596/jotcsa.1313595

View : 69 | Download : 74

Publication Date : 2023-08-30

Article Type : Research Paper

Abstract :In this study, the synthesis of chalcone compounds insert ignore into journalissuearticles values(1-11); derived from 4-insert ignore into journalissuearticles values(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 insert ignore into journalissuearticles values(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 insert ignore into journalissuearticles values(5-FU);. The best activity against PC-3 cancer cells was compound 4 insert ignore into journalissuearticles values(IC50: 1.39±0.00 µM);. In addition, compound 11 insert ignore into journalissuearticles values(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