Probing the SAR of DJ-1 using isatin-based analogs.
Compound | R1 | R2 | R3 | R4 | IC50 (μM) |
---|---|---|---|---|---|
1 | CH2CH2Ph | F | H | H | 0.118 |
2 | CH2CH2Ph | Br | H | Br | 0.0626 |
3 | CH2Ph–p-OMe | Br | H | Br | 0.267 |
4 | CH2Ph–p-Me | Br | H | Br | 0.676 |
5 | CH2Ph–p-CF3 | Br | H | Br | 2.41 |
11 | CH2Me | F | H | H | 0.118 |
12 | CH2C(C2H4)Ph | F | H | H | 0.356 |
13 | CH2CH2C(Me)3 | F | H | H | 0.851 |
14 | CH2CH2BzImzMe | F | H | H | NA |
15 | CH2CH2Ph | OMe | H | H | 2.93 |
16 | CH2CH2Ph | COOH | H | H | 9.79 |
17 | CH2CH2Ph | CH2Ph | H | H | NA |
18 | CH2Me | CH2N4 | H | H | NA |
19 | CH2CH2Ph | H | CH2COOH | H | 2.35 |
20 | CH2CH2Ph | H | H | H | 0.701 |
21 | CH2CH2Ph | F | H | OMe | 0.0546 |