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

当前位置： X-MOL 学术 › J. Heterocycl. Chem. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Novel synthesis of pyran, thiophene, and pyridine derivatives incorporating thiazole ring and their antitumor evaluation
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2019-12-26 , DOI: 10.1002/jhet.3870
Rafat M. Mohareb ₁ , Eid M. Khalil ₂ , Amany E. Mayhoub ₂ , Amira E. M. Abdallah ₂

Affiliation

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).

中文翻译：

结合噻唑环的吡喃，噻吩和吡啶衍生物的新型合成及其抗肿瘤作用

这项研究旨在设计和合成许多结合噻唑环的新型吡喃，噻吩和吡啶衍生物，并评估它们作为重要的抗癌剂的抗肿瘤抑制作用（μM）。描述了化合物1 [2-（4-氧代-4-5,5-二氢噻唑-2-基）乙腈]对不同化学试剂的反应性。此外，评估了所有新合成产物的反应性。对于所用的所有三种肿瘤癌细胞系，如MCF-7（乳腺癌），NCI-H460（非小细胞肺癌）和SF-268（CNS癌症）以及正常的成纤维细胞人类细胞系，活性最高的化合物（ WI-38）是化合物6d，8和10b与参考对照阿霉素的抗增殖作用相比。同样，某些新化合物对阿霉素所用的某些癌细胞系（例如6c（特别是对MCF-7）和2b，6b（特别是对SF-268））显示出比阿霉素更高的抑制作用。

更新日期：2019-12-27

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南11