Novel synthesis of pyran, thiophene, and pyridine derivatives incorporating thiazole ring and their antitumor evaluation

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 differ...

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Veröffentlicht in:Journal of heterocyclic chemistry 2020-03, Vol.57 (3), p.1330-1343
Hauptverfasser: Mohareb, Rafat M., Khalil, Eid M., Mayhoub, Amany E., Abdallah, Amira E. M.
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container_issue 3
container_start_page 1330
container_title Journal of heterocyclic chemistry
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creator Mohareb, Rafat M.
Khalil, Eid M.
Mayhoub, Amany E.
Abdallah, Amira E. M.
description 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).
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subjects Acetonitrile
Anticancer properties
antitumor
Biotechnology
Cancer
Derivatives
Doxorubicin
Fibroblasts
pyran
pyridine
Reagents
thiazole
thiophene
title Novel synthesis of pyran, thiophene, and pyridine derivatives incorporating thiazole ring and their antitumor evaluation
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