Synthesis, Antiproliferative Activity and In Silico Studies of Chalcones Derived From 4-(Imidazole-1-yl)Acetophenone-Reference-Cited by-同舟云学术

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

Published:2023-08-30 Issue:3 Volume:10 Page:861-868
ISSN:2149-0120
Container-title:Journal of the Turkish Chemical Society Section A: Chemistry
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Author:

KURŞUN AKTAR Bedriye Seda¹^ORCID,ALKARABASH Abdulraheem Mustafa²^ORCID,ŞAHİN YAĞLIOĞLU Ayşe³^ORCID,ORUÇ-EMRE Emine Elçin⁴^ORCID

Affiliation:

1. MALATYA TURGUT ÖZAL ÜNİVERSİTESİ YEŞİLYURT MESLEK YÜKSEKOKULU

2. CANKIRI KARATEKIN UNIVERSITY

3. AMASYA UNIVERSITY, AMASYA TECHNICAL SCIENCES VOCATIONAL SCHOOL

4. GAZIANTEP UNIVERSITY, FACULTY OF ARTS AND SCIENCES

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.

Funder

Amasya University Scientific Research Projects Governing Unit

Publisher

The Turkish Chemical Society

Subject

General Chemistry

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