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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Thiazole-containing compounds as therapeutic targets for cancer therapy
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Thiazole-containing compounds as therapeutic targets for cancer therapy

机译:含噻唑的化合物作为癌症治疗的治疗靶标

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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. (C) 2019 Elsevier Masson SAS. All rights reserved.
机译:在过去的几十年中,抗癌代理人的发展取得了相当大的进展,并制作了几种自然和合成起源的新抗癌剂。在杂环化合物中,噻唑,含有硫和氮原子的5-元独特的杂环基质,用作几种药用重要化合物中的必需核心支架。噻唑核是一些临床应用的抗癌药物的基本一部分,例如达斯替尼,Dabrafenib,Ixabopilone,Patellamide A和Epothilone。最近,已经成功地发展了含噻唑的化合物,作为几种生物靶标的可能抑制剂,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)。此外,这些化合物已被证明表现出高效率,有效的抗癌活性和毒性较小。本综述提出了目前对噻唑的研究,并阐明了他们在抗癌药物发现中的生物重要性。调查结果可以帮助研究人员更有效的设计和生物靶特异性抗癌药物分子的理性设计。 (c)2019年Elsevier Masson SAS。版权所有。

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