Ma Nan, Wang Ying, Zhao Bing-Xin, Ye Wen-Cai, Jiang Sheng
Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing, People's Republic of China ; Laboratory of Medicinal Chemistry, Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou, People's Republic of China ; Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou, People's Republic of China.
Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou, People's Republic of China.
Drug Des Devel Ther. 2015 Mar 12;9:1585-99. doi: 10.2147/DDDT.S56038. eCollection 2015.
The copper(I)-catalyzed 1,3-dipolar cycloaddition between alkynes and azides (click chemistry) to form 1,2,3-triazoles is the most popular reaction due to its reliability, specificity, and biocompatibility. This reaction has the potential to shorten procedures, and render more efficient lead identification and optimization procedures in medicinal chemistry, which is a powerful modular synthetic approach toward the assembly of new molecular entities and has been applied in anticancer drugs discovery increasingly. The present review focuses mainly on the applications of this reaction in the field of synthesis of agents with anticancer activity, which are divided into four groups: topoisomerase II inhibitors, histone deacetylase inhibitors, protein tyrosine kinase inhibitors, and antimicrotubule agents.
铜（I）催化的炔烃与叠氮化物之间的1,3-偶极环加成反应（点击化学）生成1,2,3-三唑，因其可靠性、特异性和生物相容性而成为最受欢迎的反应。该反应有可能缩短流程，并使药物化学中的先导物识别和优化流程更高效，这是一种用于组装新分子实体的强大模块化合成方法，并且越来越多地应用于抗癌药物的发现。本综述主要关注该反应在抗癌活性药物合成领域的应用，这些应用分为四类：拓扑异构酶II抑制剂、组蛋白脱乙酰酶抑制剂、蛋白酪氨酸激酶抑制剂和抗微管剂。
