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ID: ALA4270631

Journal: Eur J Med Chem

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

Authors: Tao Z, Cao R, Yan Y, Huang G, Lv K, Li W, Geng Y, Zhao L, Wang A, He Q, Yang J, Fan S, Huang M, Guo H, Zhong W, Liu M.

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.

CiteXplore: 30170321

DOI: 10.1016/j.ejmech.2018.08.057