Evaluation of Anticancer and Anti-Inflammatory Activities of some Thiazole Derivatives
CHEMISTRYSELECT, vol.11, no.32, 2026 (SCI-Expanded, Scopus)
- Publication Type: Article / Article
- Volume: 11 Issue: 32
- Publication Date: 2026
- Doi Number: 10.1002/slct.74197
- Journal Name: CHEMISTRYSELECT
- Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Chemical Abstracts Core, Academic Search Ultimate (EBSCO)
- Anadolu University Affiliated: Yes
Abstract
In this study, 2-(heteroaryl thio)-N-(4-methylthiazol-2-yl)acetamide (3a-3i) derivatives were synthesized, and the anticancer activity of the compounds were investigated on A549 lung cancer and C6 glioma cell lines. Their anti-inflammatory activities were tested against COX-1, COX-2, and LOX enzymes. Compounds 3a and 3c showed high cytotoxic activity against the A549 cell line, while compounds 3b, 3c, and 3f exhibited selective cytotoxicity against C6. Compared to cisplatin, a strong antiproliferative activity was detected against the C6 cell line. Further studies of anticancer treatments revealed that compound 3c significantly induced apoptosis, caspase-3 activation, and mitochondrial membrane polarization against the A549 cell line. Compound 3c inhibited COX-1 by 98.11% and 3h by 90.47%, while showing no significant inhibition of COX-2 or LOX. Compound 3c, a derivative containing 2-thiazoline, which showed the most potential in terms of both anticancer and anti-inflammatory activity among all compounds, was subjected to molecular docking studies on Caspase-3 and COX-1 enzymes. Compound 3c was found to interact with Ser205, Arg207, and Gly122 of caspase-3 enzyme via hydrogen bonds, and similarly, due to its hydrophobic property in both caspase-3 and COX-1 enzymes, 3c interacts with the hydrophobic regions of amino acids.