Synthesis and antiviral activities of a novel class of thioflavone and flavonoid analogues

作     者：Dajun Zhang Xingyue Ji Rongmei Gao Huiqiang Wang Shuai Meng Zhaojin Zhong Yuhuan Lin Jiandong Jiang Zhuorong Li 

作者机构：Institute of Medicinal BiotechnologyChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China 

出 版 物：《Acta Pharmaceutica Sinica B》 (药学学报（英文版）)

年 卷 期：2012年第2卷第6期

页      面：575-580页

学科分类：081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学] 

基　　金：This work was supported by the National Science and Technology Major Special Project for Major New Drugs Innovation(Item Number:2012ZX09102-101-001) 

主　　题：Thioflavones Antiviral activity Coxsackievirus Enterovirus 

摘      要：A novel class of thioflavone and flavonoid derivatives has been prepared and their antiviral activities against enterovirus 71(EV71)and the coxsackievirus B3(CVB3)and B6(CVB6)were *** 7d and 9b showed potent antiviral activities against EV71 with ICso values of 8.27 and 5.48μM,*** 7f,which has been synthesized for the first time in this work,showed the highest level of inhibitory activity against both CVB3 and CVB6 with an ICso value of 0.62 and 0.87μ*** 4b,7a,9c and 9e also showed strong inhibitory activities against both the CVB3 and CV B6 at low concentrations(IC_(50)=1.42-7.15μM),whereas compounds 4d,7c,7e and 7g showed strong activity against CVB6(IC_(50)=2.91-3.77μM)together with low levels of activity against *** 7d exhibited stronger inhibitory activity against CVB3(IC_(50)=6.44μM)thaln CVB6(IC_(50)8.29μM).The thioflavone derivatives 7a,7c,7d,7e,7f and 7g,represent a new class of lead compounds for the development of novel antiviral agents.