TABLE 1.
Inhibitory activities of 2,5-substituted furan derivatives 1a–k against PRMT1.
| |||||
| Cpd no. | Cpd ID. | R1 | R 2 | % Inhibition of PRMT1 (at 10 μM) a | IC50 (μM) |
| — | SAH | — | — | — | 0.55 ± 0.07 |
| — | DB75 | — | — | 98.13 ± 0.27 | 0.31 ± 0.04 |
| 1a | ZZQ-16 | H | -CONH2 | 10.61 ± 2.24 | — |
| 1b | ZZQ-82 | H | -CONHNH2 | 48.00 ± 0.02 | — |
| 1c | ZZQ-55 | H | -NH2 | 50.00 ± 0.18 | 21.42 ± 12.76 |
| 1d | ZZQ-52 | -NH2 | H | 35.99 ± 0.09 | — |
| 1e | ZZQ-102 | H |
|
32.00 ± 0.00 | — |
| 1f | ZZQ-127 | F |
|
35.97 ± 0.20 | — |
| 1g | ZZQ-100 |
|
H | 39.98 ± 0.19 | — |
| 1h | SYT-302 | H |
|
74.54 ± 0.16 | 2.66 ± 0.01 |
| 1i | SYT-298 | F |
|
68.00 ± 0.02 | 4.42 ± 0.63 |
| 1j | SYT-290 |
|
H | 76.82 ± 1.19 | 2.06 ± 0.60 |
| 1k | SYT309 |
|
Cl | 76.50 ± 0.01 | 2.50 ± 0.91 |
Initial inhibition rate was tested at 10 μM for all compounds, and only those with >50% inhibition effects were selected for IC50 measurements.