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Novel synthesis of pyran,thiophene, and pyridine derivatives incorporating thiazole ring and their antitumor evaluation
Authors:Rafat M Mohareb  Eid M Khalil  Amany E Mayhoub  Amira E M Abdallah
Institution:1. Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt;2. Department of Chemistry, Faculty of Science, Helwan University, Helwan, Egypt
Abstract:This study aims to design and synthesize a number of novel pyran, thiophene, and pyridine derivatives incorporating thiazole ring and evaluate their antitumor inhibition (μM) as significant anticancer agents. The reactivity of compound 1 2-(4-oxo-4,5-dihydrothiazol-2-yl)acetonitrile] towards different chemical reagents was described. Furthermore, the reactivity of all the newly synthesized products was evaluated. The most active compounds towards all the three tumor cancer cell lines used such as MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) and SF-268 (CNS cancer), and normal fibroblasts human cell line (WI-38) were compounds 6d , 8 , and 10b , which compared with the antiproliferative effects of the reference control doxorubicin. Also, some of the novel compounds indicate higher inhibition than doxorubicin against some of the cancer cell lines used such as 6c (especially towards MCF-7) and 2b , 6b (especially towards SF-268).
Keywords:antitumor  pyran  pyridine  thiazole  thiophene
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