Table 2.
EC50 values for reference compounds GCV, ART, ARN, DHA, artemether, tenofovir alafenamide fumarate (TAF); parent compound 13; and hybrids 1–12, which were analyzed for anti‐HCMV and anti‐HBV activities.[a]
|
Compound |
HCMV EC50 [μm] |
LDH CC50 [μm] |
HepG2‐hNTCP CC50 [μm] |
HBeAg ELISA EC50 [μm] |
HBV DNA qPCR EC50 [μm] |
|---|---|---|---|---|---|
|
1 |
0.22±0.04 |
>100* |
29.9±1.1 |
2.57±1.51 |
≈10 |
|
2 |
0.67±0.03 |
>100 |
>50 |
>10 |
>10 |
|
3 |
none |
>100 |
n.d. |
n.d. |
n.d. |
|
4 |
none (strong cytotox. **) |
>100** |
n.d. |
n.d. |
n.d. |
|
5 |
none (strong cytotox. **) |
>100** |
>50 |
>10 |
>10 |
|
6 |
none (strong cytotox. **) |
>100** |
n.d. |
n.d. |
n.d. |
|
7 |
none (strong cytotox. **) |
>100** |
>50 |
>10 |
>10 |
|
8 |
0.71±0.03 |
n.d. |
n.d. |
n.d. |
n.d. |
|
9 |
1.20±0.11 |
>100 |
n.d. |
n.d. |
n.d. |
|
10 |
1.08±0.18 |
>100* |
n.d. |
n.d. |
n.d. |
|
11 |
0.30±0.02 |
>100 |
>50 |
>10 |
>10 |
|
12 |
0.38±0.03 |
>100 |
>50 |
>10 |
>10 |
|
13 |
>10 |
n.d. |
n.d. |
n.d. |
n.d. |
|
ARN[b] |
>10 |
>100 |
n.d. |
n.d. |
n.d. |
|
ART[c] |
5.41±0.61 |
n.d. |
>50 |
>10 |
>10 |
|
DHA[b] |
>10 |
n.d. |
>50 |
>10 |
>10 |
|
artemether |
>10 |
>100 |
n.d. |
n.d. |
n.d. |
|
GCV[d] |
2.60±0.5 |
>100 |
n.d. |
n.d. |
n.d. |
|
TAF |
– |
– |
27.2±0.7 |
3.93±0.8 |
0.00024±0.00004 |
[a] */** Microscopic inspection of cell morphology or cell lysis after 6–8 days, long‐term cytotoxicity (* moderate, ** strong). LDH: lactate dehydrogenase release assay, 24 h, acute cytotoxicity; “n.d.”—not determined. [b] EC50 values have been previously reported.6a, 29 [c] EC50 values have been previously reported.30 [d] EC50 values have been previously reported.31