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含噻唑的化合物作为癌症治疗的治疗靶点。

Thiazole-containing compounds as therapeutic targets for cancer therapy.

机构信息

Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra, HR, 136119, India.

Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra, HR, 136119, India.

出版信息

Eur J Med Chem. 2020 Feb 15;188:112016. doi: 10.1016/j.ejmech.2019.112016. Epub 2019 Dec 28.

Abstract

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.

摘要

在过去的几十年中,抗癌药物的开发取得了相当大的进展,已经生产出了几种天然和合成来源的新型抗癌药物。在杂环化合物中,噻唑是一种含有硫和氮原子的 5 元独特杂环基序,是几种具有重要药用价值的化合物的基本核心支架。噻唑核是一些临床应用的抗癌药物的基本部分,如 dasatinib、dabrafenib、ixabepilone、patellamide A 和 epothilone。最近,噻唑类化合物已成功开发为几种生物靶标的潜在抑制剂,包括位于细胞膜上的酶联受体(如聚合酶抑制剂)和细胞周期(如微管抑制剂)。此外,这些化合物已被证明具有高效、强大的抗癌活性和较低的毒性。本综述介绍了噻唑类化合物的最新研究进展,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生物靶向特异性的抗癌药物分子。

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