Table 1.
Compd | Type | X | R2 | R4 | R1 | IC50 [μm][a] |
---|---|---|---|---|---|---|
7 a | I | O | H | H | 2-Me | 230 |
1 b | I | O | Et | H | 2-Me | 24 |
7 b | I | O | Cl | H | 2-Me | 176 |
7 c | – | – | – | – | – | NA |
7 d | I | O | H | Me | 2-Me | 88 |
7 e | I | O | H | Cl | 2-Me | 710 |
7 f | I | O | H | OMe | 2-Me | 122 |
7 g | I | O | H | iPr | 2-Me | 27 |
7 h | I | NH | H | Cl | 4-Me | NA |
1 c | I | NH | H | Me | 4-OMe | 90 |
7 i | I | NH | Et | H | 4-OMe | 75 |
6 a | II | NH | Et | H | 4-OMe | NA |
6 b | II | NH | H | Me | 4-OMe | 35 |
6 c | II | NH | H | Cl | 4-Me | 115 |
6 d | II | O | H | H | 2-Me | 481 |
6 e | II | O | Et | H | 2-Me | 275 |
6 f | II | O | Cl | H | 2-Me | 83 |
6 g | – | – | – | – | – | 117 |
6 h | II | O | H | Cl | 2-Me | 23 |
6 i | II | O | H | Me | 2-Me | partial |
6 j | II | O | H | OMe | 2-Me | partial |
6 k | II | O | H | iPr | 2-Me | 68 |
[a] NA: no inhibition was observed; partial: compound behaved as partial blocker of binding.