Tao, ZeyuCao, RuiyuanYan, YunzhengHuang, GuochengLv, KaiLi, WeiGeng, YunheZhao, LeiWang, ApengHe, QinhaoYang, JingjingFan, ShiyongHuang, MenghaoGuo, HuiyuanZhong, WuLu, Mingliang2018-10-052018-10-052018-09Tao, Z., Cao, R., Yan, Y., Huang, G., Lv, K., Li, W., ... & Yang, J. (2018). Design, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives. European journal of medicinal chemistry, 157, 994-1004. https://doi.org/10.1016/j.ejmech.2018.08.057https://hdl.handle.net/1805/17471We report herein the design and synthesis of a series of novel Sinefungin (SIN) derivatives, based on the structures of SIN and its analogue EPZ004777. Our results reveal that target compounds 1ad-af, 1ba-bb and 1bf-bh show better activity (IC50 = 4.56–20.16 μM) than EPZ004777 (IC50 = 35.19 μM). Surprisingly, SIN was founded to be not as active (IC50 > 50 μM) as we and other research groups predicted. Interestingly, the intermediates 9a-b and 11b display potent anti-ZIKV potency (IC50 = 6.33–29.98 μM), and compound 9a also exhibits acceptable cytotoxicity (CC50 > 200 μM), suggesting their promising potential to be leads for further development.enPublisher Policyanti-Zika virusSinefunginEPZ004777,Article