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Thiazole-containing compounds as therapeutic targets for cancer therapy.
European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2019-12-28 , DOI: 10.1016/j.ejmech.2019.112016
Prabodh Chander Sharma 1 , Kushal Kumar Bansal 1 , Archana Sharma 1 , Diksha Sharma 1 , Aakash Deep 2
Affiliation  

In the last few decades, considerable progress has been made in anticancer agents development, and several new anticancer agents of natural and synthetic origin have been produced. Among heterocyclic compounds, thiazole, a 5-membered unique heterocyclic motif containing sulphur and nitrogen atoms, serves as an essential core scaffold in several medicinally important compounds. Thiazole nucleus is a fundamental part of some clinically applied anticancer drugs, such as dasatinib, dabrafenib, ixabepilone, patellamide A, and epothilone. Recently, thiazole-containing compounds have been successfully developed as possible inhibitors of several biological targets, including enzyme-linked receptor(s) located on the cell membrane, (i.e., polymerase inhibitors) and the cell cycle (i.e., microtubular inhibitors). Moreover, these compounds have been proven to exhibit high effectiveness, potent anticancer activity, and less toxicity. This review presents current research on thiazoles and elucidates their biological importance in anticancer drug discovery. The findings may aid researchers in the rational design of more potent and bio-target specific anticancer drug molecules.

中文翻译:

含噻唑化合物作为癌症治疗的治疗靶标。

在过去的几十年中,抗癌剂的开发取得了相当大的进步,并且已经生产了几种天然和合成来源的新型抗癌剂。在杂环化合物中,噻唑(一种含有硫和氮原子的5元独特的杂环基序)在几种具有医学重要性的化合物中用作必不可少的核心骨架。噻唑核是一些临床应用的抗癌药物的基本组成部分,例如达沙替尼,达布拉非尼,依沙贝比隆,pa酰胺A和埃坡霉素。最近,已成功开发出含噻唑的化合物作为几种生物学靶标的可能抑制剂,包括位于细胞膜上的酶联受体(即聚合酶抑制剂)和细胞周期(即微管抑制剂)。而且,这些化合物已被证明具有很高的效力,有效的抗癌活性和较低的毒性。这篇综述介绍了目前对噻唑的研究,并阐明了它们在抗癌药物发现中的生物学重要性。这些发现可能有助于研究人员合理设计更有效和更具生物靶向性的抗癌药物分子。
更新日期:2019-12-29
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