Laboratory of Chemistry and Biodiversity, School of Life Science and Engineering, Southwest Jiaotong University, Chengdu, 610031, PR China.
Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu, 610041, PR China.
Eur J Med Chem. 2019 Nov 15;182:111664. doi: 10.1016/j.ejmech.2019.111664. Epub 2019 Aug 30.
As an important source of drugs, natural products play an important role in the discovery and development of new drugs. More than 60% of anti-tumor drugs are closely related to natural products. At the same time, as the main cause of tumors, the abnormal activity of tyrosine kinase has become an important target for clinical treatment. Although, small molecule targeted drugs dominate the cancer treatment. Natural active products are driving the development of new tyrosine kinase inhibitors with their unique mode of action and molecular structure diversity. Obtaining new chemical entities with tyrosine kinase inhibitory activity from natural active products will bring new breakthroughs in the research of anticancer drugs. In this paper, different tyrosine kinases are mainly classified as targets, and natural products and derivatives which have been found to inhibit tyrosine kinase activity have been described. It is hoped that by analyzing the different aspects of the source, structural characteristics, mechanism of action and biological activity of these natural products, we will find new members that can be developed into drugs and promote the development of anti-tumor drugs.
天然产物作为药物的重要来源，在新药的发现和开发中发挥着重要作用。超过 60%的抗肿瘤药物与天然产物密切相关。同时，作为肿瘤的主要成因，酪氨酸激酶的异常活动已成为临床治疗的重要靶点。尽管小分子靶向药物主导着癌症治疗，但天然活性产物以其独特的作用模式和分子结构多样性推动着新型酪氨酸激酶抑制剂的发展。从天然活性产物中获得具有酪氨酸激酶抑制活性的新化学实体将为抗癌药物的研究带来新的突破。本文主要将不同的酪氨酸激酶分类为靶点，并描述了已发现具有抑制酪氨酸激酶活性的天然产物及其衍生物。希望通过分析这些天然产物在来源、结构特征、作用机制和生物活性等不同方面的特点，找到可以开发成药物的新成员，从而促进抗肿瘤药物的发展。
