Synthesis and biological evaluation of 5-methyl-4-phenyl thiazole derivatives as anticancer agents |
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Authors: | Asaf E Evren Leyla Yurttas Bü?ra Ekselli Gül?en Akalin-Ciftci |
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Institution: | 1. Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Anadolu University, Eski?ehir, Turkey;2. asafevrimevren@anadolu.edu.tr;4. Faculty of Pharmacy, Department of Biochemistry, Anadolu University, Eski?ehir, Turkey |
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Abstract: | AbstractNew N-(5-methyl-4-phenylthiazol-2-yl)-2-(substituted thio)acetamides were synthesized and studied for their anticancer activity. The title compounds were procured by reacting 2-chloro-N-(5-methyl-4-phenylthiazol-2-yl)acetamide with some mercapto derivatives. The structural elucidation of the compounds was performed by 1H-NMR, 13C-NMR and LC-MS/MS spectral data and elemental analyses. The synthesized compounds were investigated for their antitumor activities against A549 human lung adenocarcinoma cells and NIH/3T3 mouse embryoblast cell line for determining their selective cytotoxicity. 2-(1-methyl-1H-tetrazol-5-yl)thio]-N-(5-methyl-4-phenylthiazol-2-yl)acetamide (4c) showed high selectivity, and whose IC50 value was determined as 23.30?±?0.35?µM and >1000?µM against A549 human lung adenocarcinoma cells and NIH/3T3 mouse embryoblast cell lines, respectively. 2-(1-Methyl-1H-imidazol-2-yl)thio]-N-(5-methyl-4-phenyl thiazol-2-yl)acetamide (4a) and 2-(1-Methyl-1H-tetrazol-5-yl)thio]-N-(5-methyl-4-phenyl thiazol-2-yl)acetamide (4c) exhibited the highest apoptosis percentage among those tested, but not as high as the standard, cisplatin. |
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Keywords: | Azoles anticancer activity thiazole apoptosis |
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