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黄酮类化合物靶向丝氨酸/苏氨酸蛋白激酶作为潜在抗癌药物的研究进展。

A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.

机构信息

Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, People's Republic of China.

Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, People's Republic of China.

出版信息

Bioorg Med Chem. 2019 Mar 1;27(5):677-685. doi: 10.1016/j.bmc.2019.01.027. Epub 2019 Jan 26.

Abstract

Protein kinases have been important targets for antitumor targets due to their key roles in regulating multiple cell signaling pathways. Numerous compounds containing flavonoid scaffold as an indispensable anchor have been found to be potent inhibitors of protein kinases. Some of these flavonoids have been in clinical research as protein kinases inhibitors. Thus, the present review mainly focuses on the structural requirement for anticancer potential of flavone derivatives targeting several key serine/threonine protein kinases. This information may provide an opportunity to scientists of medicinal chemistry to design multi-functional flavone derivatives for the treatment of cancer.

摘要

蛋白激酶因其在调节多种细胞信号通路中的关键作用而成为抗肿瘤药物的重要靶点。已经发现许多含有黄酮骨架作为不可或缺的锚点的化合物是蛋白激酶的有效抑制剂。其中一些黄酮类化合物已作为蛋白激酶抑制剂进行临床研究。因此,本综述主要集中于针对几种关键丝氨酸/苏氨酸蛋白激酶的具有抗癌潜力的黄酮衍生物的结构要求。这些信息可能为药物化学科学家提供设计用于治疗癌症的多功能黄酮衍生物的机会。

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