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Design, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives. 2018
Zeyu Tao, and
Ruiyuan Cao, and
Yunzheng Yan, and
Guocheng Huang, and
Kai Lv, and
Wei Li, and
Yunhe Geng, and
Lei Zhao, and
Apeng Wang, and
Qinghao He, and
Jingjing Yang, and
Shiyong Fan, and
Menghao Huang, and
Huiyuan Guo, and
Wu Zhong, and
Mingliang Liu
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China.
We 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.
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