Table 1.
Activity of 7-substituted 1-hydroxy-3,7-dihydro-1H-purine-2,6-diones 5
| Cmpd |  |
IC50 (μM)a (Caf1) | IC50 (μM)a (PARN) |
|---|---|---|---|
| 5a |  |
10.4 ± 0.4 | 84.1 ± 6.7 |
| 5b |  |
28.2 ± 7.6 | n.d. |
| 5c |  |
10.6 ± 2.7 | 119 ± 25 |
| 5d |  |
6.6 ± 0.7 | 125 ± 32 |
| 5e |  |
23.3 ± 2.2 | 245 ± 20 |
| 5f |  |
13.3 ± 2.3 | n.d. |
| 5g |  |
20.6 ± 5.8 | n.d. |
| 5h |  |
3.6 ± 1.1 | n.d. |
| 5i |  |
10.6 ± 4.3 | n.d. |
| 5j |  |
1.5 ± 0.3 | n.d. |
| 5k |  |
4.0 ± 1.1 | n.d. |
a
IC50 values were determined using a fluorescence-based biochemical assay as described.22 Also indicated are the standard errors of the means (n = 3). N.d., not determined.