Selected article for: "cell virus and infected cell"
Author: Linlin Zhang; Daizong Lin; Yuri Kusov; Yong Nian; Qingjun Ma; Jiang Wang; Albrecht von Brunn; Pieter Leyssen; Kristina Lanko; Johan Neyts; Adriaan de Wilde; Eric J. Snijder; Hong Liu; Rolf Hilgenfeld
Title: Alpha-ketoamides as broad-spectrum inhibitors of coronavirus and enterovirus replication
  • Document date: 2020_2_10
    • ID: 7n8p9okf_11
    Snippet: The initial compound to be designed and synthesized was 11a, which carries a cinnamoyl N-cap in the P3 position, a benzyl group in P2, the glutamine lactam (GlnLactam) in P1, and benzyl in P1' (Table 1) . This compound showed good to mediocre activities against recombinant SARS-CoV M pro (IC50 = 1.95 µM; for all compounds, see Tables 1 -3 for standard deviations), CVB3 3C pro (IC50 = 6.6 µM), and EV-A71 3C pro (IC50 = 1.2 µM), but was surpris.....
    Document: The initial compound to be designed and synthesized was 11a, which carries a cinnamoyl N-cap in the P3 position, a benzyl group in P2, the glutamine lactam (GlnLactam) in P1, and benzyl in P1' (Table 1) . This compound showed good to mediocre activities against recombinant SARS-CoV M pro (IC50 = 1.95 µM; for all compounds, see Tables 1 -3 for standard deviations), CVB3 3C pro (IC50 = 6.6 µM), and EV-A71 3C pro (IC50 = 1.2 µM), but was surprisingly completely inactive (IC50 > 50 µM) against HCoV-NL63 M pro . These values were mirrored in the SARS-CoV and in the enterovirus replicons (Table 2) . In virus-infected cell cultures, the results obtained were also good to mediocre (Table 3) : SARS-CoV (EC50 = 5.8 µM in Vero E6 cells), MERS-CoV (EC50 = 0.0047 µM in Huh7 cells), HCoV 229E (EC50 = 11.8 µM in Huh7 cells), or a host of enteroviruses (EC50 = 9.8 µM against EV-A71 in RD cells; EC50 = 0.48 µM against EV-D68 in HeLa Rh cells; EC50 = 5.6 µM against HRV2 in HeLa Rh cells). In all cell types tested, the compound generally proved to be non-toxic, with selectivity indices (CC50/EC50) usually >10 (Table 3) .

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