LitCovid-sentences  

PMC:7291971 / 22613-25169 JSONTXT 9 Projects

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Id Subject Object Predicate Lexical cue
T158 0-197 Sentence denotes To confirm the observed inhibition of some adenine dinucleosides against SARS-CoV nsp14 N7-MTase, we further tested 10 compounds in a dose-response assay (Table 2 , Supporting Information Fig. S2).
T159 198-321 Sentence denotes The selection of these compounds was based on their percentage inhibition higher than 50% against SARS-CoV nsp14 (Table 1).
T160 322-431 Sentence denotes After pre-incubation with increasing concentrations of dinucleosides, the MTase activity was measured by FBA.
T161 432-626 Sentence denotes The IC50 of compounds, deduced from Hill slope equation (Y = 100/(1+((X/IC50)^Hillslope) curve-fitting, ranged from 0.6 μM to 70.4 μM on SARS-CoV nsp14 and 10.9 μM to > 500 μM on hRNMT activity.
T162 627-881 Sentence denotes Among all the potential inhibitors, three compounds 2, 6 and 11 showed the lowest inhibitory activity on SARS-CoV nsp14 with IC50 > 40 μM, the others have IC50 values in the micromolar range except 13 that showed an IC50 value in the submicromolar range.
T163 882-999 Sentence denotes The potency of the derivative 13 to inhibit SARS-CoV nsp14 was comparable to the broad spectrum inhibitor sinefungin.
T164 1000-1204 Sentence denotes However, it is noteworthy that compound 13 specifically inhibits the N7-MTase of SARS-CoV with a high 413-fold of specificity in dose-response testing whereas sinefungin is also active against hRNMT [11].
T165 1205-1505 Sentence denotes Remarkably 13 bearing a chlorine atom in “para” position and a nitro group in “meta” position displayed the best inhibition which was 6.5–9.5 fold more potent than the derivatives 10 and 12, respectively that contain the nitro in “ortho” position and a lipophilic group CF3 or MeO in “para” position.
T166 1506-1665 Sentence denotes The comparison of IC50 values of 14 and 13 indicates that the addition of a nitro group in the phenyl ring increased the inhibitory activity by 2.5 fold in 13.
T167 1666-1830 Sentence denotes These results confirm that the chlorine atom in “para” position and the presence of a nitro group seem crucial for submicromolar SARS-CoV nsp14 inhibitory activity.
T168 1831-1937 Sentence denotes Table 2 Comparison of IC50 values of 10 most active compounds on SARS-CoV nsp14 and human RNMT activities.
T169 1938-1988 Sentence denotes Compounds SARS-CoV nsp14 IC50a (μM) hRNMTIC50 (μM)
T170 1989-2011 Sentence denotes Sinefunginb 0.36 <0.05
T171 2012-2035 Sentence denotes 2 40.6 ± 3.2 10.9 ± 1.0
T172 2036-2053 Sentence denotes 6 55.5 ± 5.1 >500
T173 2054-2070 Sentence denotes 9 2.6 ± 0.2 >500
T174 2071-2088 Sentence denotes 10 3.9 ± 0.4 >500
T175 2089-2115 Sentence denotes 11 70.4 ± 4.9 169.3 ± 30.4
T176 2116-2141 Sentence denotes 12 5.7 ± 0.5 275.9 ± 28.7
T177 2142-2167 Sentence denotes 13 0.6 ± 0.1 247.5 ± 14.9
T178 2168-2184 Sentence denotes 14 1.5 ± 0.1 n.d
T179 2185-2201 Sentence denotes 15 2.4 ± 0.2 n.i
T180 2202-2218 Sentence denotes 16 9.9 ± 0.9 n.d
T181 2219-2315 Sentence denotes a Concentration inhibiting MTase activity by 50%; mean value from three independent experiments.
T182 2316-2350 Sentence denotes b values from the literature [11].
T183 2351-2556 Sentence denotes The MTase activity for IC50 determinations was measured using a filter binding assay as described above. n.i: no inhibition detected at 50 μM; n.d: not determined due to inhibition lower than 50% at 50 μM.