Thiazole moiety: A promising scaffold for anticancer drug discovery

• Published in: Journal of molecular structure Vol. 1303; p. 137510
• Main Authors: Kassem, Asmaa F., Althomali, Raed H., Anwar, Manal M., El-Sofany, Walaa I.
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 05.05.2024
• Subjects: Anticancer; Enzyme inhibitors; Heterocyclic compound; Molecular docking; Synthesis; Thiazoles; Synthesis; Enzyme inhibitors; Anticancer; Heterocyclic compound; Molecular docking; Thiazoles
• ISSN: 0022-2860; 1872-8014
• DOI: 10.1016/j.molstruc.2024.137510

•Biological activities of thiazole-containing compounds.•Synthesis of 1, 3-thiazole derivatives.•Important enzymatic pathway in carcinogenesis.•Thiazole derivatives as EGFR kinase inhibitors.•Thiazole derivatives as Akt (PKB) protein kinase inhibitors.•Thiazole derivatives as Tubulin polymerization inhibitors.•Thiazole derivatives as VEGF (Vascular Endothelial Growth Factor) inhibitors. Over the past few decades, significant advancements in the discovery of anticancer medicines have yielded various novel agents, both synthetic and natural in origin. Thiazoles are a special type of heterocyclic compound with five members that comprise nitrogen and sulfur atoms. These compounds are vital core scaffolds in a number of significant pharmaceutical drugs including anticancer. It was discovered that several chemotherapy drugs have some naturally occurring chemicals and a thiazole nucleus. Some clinically used anticancer medications have thiazole nucleus as a basic component including Vosaroxin, Dabrafenib, patellamide A, dasatinib, epothilones, ixabepilone, tiazofurin, Kud 773, and bleomycin. Recently, thiazole-containing compounds have been effectively developed as possible inhibitors of several anti-cancer targets, including enzyme-linked receptor(s) found on the cell membrane (i.e., polymerase inhibitors) and the cell cycle (i.e., microtubular inhibitors). Additionally, it has been demonstrated that these substances exhibit low toxicity, strong anticancer activity, and great efficacy. The biological importance of thiazoles in the creation of anticancer medications is discussed in this article, which also reviews recent research on the subject. The results may help in the development of more potent and precisely tailored anticancer medications.