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. Author manuscript; available in PMC: 2018 Sep 13.
Published in final edited form as: Bioorg Med Chem Lett. 2013 Dec 9;24(2):609–612. doi: 10.1016/j.bmcl.2013.12.012

Table 1.

Helicase inhibition and viral replication inhibition data for UK-1 and analogs 1-6.

Compound Helicasea
Repliconc,d
DNA RNA

IC50(μM)b IC50(μM)b EC50 (μM)e CC50 (μM)f SI50g
UK-1 380 >1200 0.77 17 22
1 >1800 >1800 0.50 5.4 11
2 >1800 >1800 0.53 3.5 6.6
3 >1800 >1800 1.4h 6.3h 4.5h
4 540 590 0.53 2.5 4.7
5 3.8 20 2.1 >20 >10
6 2.6 20 0.54 >20 >37
a

Strand separation of radiolabeled oligonucleotides was monitored using gel electrophoresis (see Supplemental Information).

b

The concentration of compound required to inhibit 50% of helicase activity.

c

Experiments were carried out at Southern Research Institute, Frederick, MD.

d

Results are the averages of 2–4 independent dose-response experiments using a combination of luciferase reporter-based and RNA assays unless noted.

e

The concentration of compound that inhibits 50% of viral RNA replication.

f

The concentration of compound that kills 50% of the cells.

g

The ratio of EC50 to CC50.

h

Result is from a single luciferase reporter-based assay.