Table 1. MDM2 structure–activity relationships for purchased pyrroles 4a–l .
| |||||
Compound | R1 | R2 | R3 | R4 | MDM2 IC50 (nM) |
4a | 4-ClPh | Me | H | H | 720 ± 100 |
4b | 4-ClPh | Me | H | Ph | 3300 ± 700 |
4c | 4-ClPh | Ph | H | H | 120 ± 20 |
4d | 4-ClPh | Ph | H | Ph | 230 ± 44 |
4e | 4-ClPh | Ph | H | 3-ClPh | 163 ± 17 |
4f | 4-ClPh | Ph | 3,4-diMePh | Ph | 256 ± 39 |
4g | 4-ClPh | Ph | Me | Me | Insol. |
4h | 4-BrPh | Me | Ph | Ph | 199 ± 16 |
4i | 4-MePh | Me | H | Ph | 8400 ± 900 |
4j | 4-MePh | Me | H | H | 4700 ± 200 |
4k | 4-EtO2CPh | Ph | H | H | 700 ± 20 |