Design, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives
dc.contributor.author | Tao, Zeyu | |
dc.contributor.author | Cao, Ruiyuan | |
dc.contributor.author | Yan, Yunzheng | |
dc.contributor.author | Huang, Guocheng | |
dc.contributor.author | Lv, Kai | |
dc.contributor.author | Li, Wei | |
dc.contributor.author | Geng, Yunhe | |
dc.contributor.author | Zhao, Lei | |
dc.contributor.author | Wang, Apeng | |
dc.contributor.author | He, Qinhao | |
dc.contributor.author | Yang, Jingjing | |
dc.contributor.author | Fan, Shiyong | |
dc.contributor.author | Huang, Menghao | |
dc.contributor.author | Guo, Huiyuan | |
dc.contributor.author | Zhong, Wu | |
dc.contributor.author | Lu, Mingliang | |
dc.contributor.department | Medicine, School of Medicine | en_US |
dc.date.accessioned | 2018-10-05T17:07:05Z | |
dc.date.available | 2018-10-05T17:07:05Z | |
dc.date.issued | 2018-09 | |
dc.description.abstract | 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. | en_US |
dc.eprint.version | Author's manuscript | en_US |
dc.identifier.citation | Tao, 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.2018.08.057 | en_US |
dc.identifier.uri | https://hdl.handle.net/1805/17471 | |
dc.language.iso | en | en_US |
dc.publisher | Elsevier | en_US |
dc.relation.isversionof | 10.1016/j.ejmech.2018.08.057 | en_US |
dc.relation.journal | European Journal of Medicinal Chemistry | en_US |
dc.rights | Publisher Policy | en_US |
dc.source | Author | en_US |
dc.subject | anti-Zika virus | en_US |
dc.subject | Sinefungin | en_US |
dc.subject | EPZ004777, | en_US |
dc.title | Design, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives | en_US |
dc.type | Article | en_US |