Design, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives

European Journal of Medicinal Chemistry
Zeyu TaoMingliang Liu

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.

Citations

Oct 3, 2020·Bioorganic & Medicinal Chemistry·Leandro Rocha SilvaEdeildo Ferreira da Silva-Júnior
Jul 7, 2020·Organic Letters·Ludovic DecultotMatthew D Shair
Apr 27, 2021·Frontiers in Cellular and Infection Microbiology·Weibao SongJiandong Jiang
Sep 25, 2019·Journal of Medicinal Chemistry·Jean A BernatchezRongshi Li
Jan 28, 2020·Journal of Chemical Information and Modeling·Felipe R S SantosJaqueline M S Ferreira
Dec 15, 2021·The Journal of Organic Chemistry·Dellamol SebastianMahesh K Lakshman

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