Table 1. PSMA Inhibitory Activity of Compounds 7a–c, 8a–b, 9a–b, 10, 9a–b, 12, 13a–b, 14, 15, 21a–b, and 22a–ba.
| compd | IC50 (nM) | compd | IC50 (nM) |
|---|---|---|---|
| 7a | 2.32 ± 0.55 | 12 | 0.20 ± 0.11 |
| 7b | 2.91 ± 0.33 | 13a | 0.99 ± 0.05 |
| 7c | 2.11 ± 1.01 | 13b | 0.075 ± 0.005 |
| 8a | 0.64 ± 0.07 | 14 | 1.31 ± 0.18 |
| 8b | 0.46 ± 0.10 | 15 | 1.19 ± 0.73 |
| 9a | 5.24 ± 1.45 | 21a | 0.94 ± 0.26 |
| 9b | 5.44 ± 2.54 | 21b | 0.15 ± 0.02 |
| 10 | 4.46 ± 1.03 | 22a | 1.11 ± 0.22 |
| 11a | 0.35 ± 0.01 | 22b | 0.13 ± 0.01 |
| 11b | 0.28 ± 0.09 | 16 (DCIBzL) | 0.021 ± 0.004 |
Inhibition constants of studied compounds were determined using the radioenzymatic assay with [3H]NAAG (radiolabeled at the terminal glutamate) as described previously.22