Author: Rui Xiong; Leike Zhang; Shiliang Li; Yuan Sun; Minyi Ding; Yong Wang; Yongliang Zhao; Yan Wu; Weijuan Shang; Xiaming Jiang; Jiwei Shan; Zihao Shen; Yi Tong; Liuxin Xu; Chen Yu; Yingle Liu; Gang Zou; Dimitri Lavillete; Zhenjiang Zhao; Rui Wang; Lili Zhu; Gengfu Xiao; Ke Lan; Honglin Li; Ke Xu
Title: Novel and potent inhibitors targeting DHODH, a rate-limiting enzyme in de novo pyrimidine biosynthesis, are broad-spectrum antiviral against RNA viruses including newly emerged coronavirus SARS-CoV-2 Document date: 2020_3_12
ID: hq5um68k_15
Snippet: Additionally, S312 and S416 exhibited ideal antiviral efficacies of EC50=1.55μM (SI>64.62) and EC50=0.017μM (extensively high SI>5882.4), respectively ( Fig. 2C lower panel). Compared with our previous publication of Remdesivir (EC50=0.77μM, SI>129.87) and Chloroquine (EC50=1.13μM, SI>88.5) 29 , which are currently used in clinical trials against SARS-CoV-2, S416 had much greater EC50 and SI values (66.5fold stronger than Chloroquine in EC50).....
Document: Additionally, S312 and S416 exhibited ideal antiviral efficacies of EC50=1.55μM (SI>64.62) and EC50=0.017μM (extensively high SI>5882.4), respectively ( Fig. 2C lower panel). Compared with our previous publication of Remdesivir (EC50=0.77μM, SI>129.87) and Chloroquine (EC50=1.13μM, SI>88.5) 29 , which are currently used in clinical trials against SARS-CoV-2, S416 had much greater EC50 and SI values (66.5fold stronger than Chloroquine in EC50) against SARS-CoV-2. The data in Fig. 2D clearly showed that as little as 4.6nM (0.3EC50) of S416 can dramatically inhibit SARS-CoV-2 infections, while, increased drug concentration of 370nM (22EC50) could further eliminate viral infected cells. Thus, S416 turns to be the best efficient chemical so far against SARS-CoV-2 at the cellular level.
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