Compounds | N | Y | X | R | R′ | IC50 (μM)a |
---|---|---|---|---|---|---|
Sorbinil | 0.65 | |||||
1b | 0 | CO | H | 4-OMe-Ph | H | 2.25 |
2b | 0 | CO | Br | 4-OMe-Ph | H | 0.58 |
3 | 1 | CO | H | 4-OMe-Ph | Me | n.a. |
4 | 1 | CO | Br | 4-OMe-Ph | Me | 4.97 |
5 | 0 | CO | H | Me | Me | 42.3 |
6 | 0 | CO | Br | Me | Me | 17.3 |
7 | 1 | CO | H | Me | Me | 2.00 |
8 | 1 | CO | Br | Me | Me | n.a. |
9 | 1 | CH2 | H | Me | Me | n.a. |
10 | 1 | CH2 | Br | Me | Me | 4.17 |