Table 1.
No. | R1 | R2 | R3 | Inhibition rate (1 μmol/L/10 μmol/L, %)a |
|||||
---|---|---|---|---|---|---|---|---|---|
PARP1 (μmol/L) |
BRD4 (μmol/L) |
||||||||
1 | 10 | 1 | 10 | ||||||
5a | 4,6-diOCH3 | CONHCH3 | – | 4 | 25 | 1 | 36 | ||
5b | H | CONHCH3 | – | 0 | 15 | 0 | 22 | ||
5c | 4,6-diOCH3 | CONH2 | – | 0 | 2 | 1 | 18 | ||
5d | H | CONH2 | – | 0 | 1 | 2 | 19 | ||
5e | 4,6-diOCH3 | – | 2 | 36 | 12 | 70 | |||
5f | H | – | 0 | 29 | 12 | 55 | |||
5g | 4,6-diOCH3 | – | 9 | 34 | 3 | 13 | |||
5h | H | – | 3 | 10 | 0 | 11 | |||
5i | 4,6-diOCH3 | – | 8 | 31 | 7 | 60 | |||
5j | H | – | 7 | 28 | 6 | 26 | |||
5k | 4,6-diOCH3 | – | 6 | 39 | 8 | 42 |
‒Not applicable.
Each compound was tested in duplicate, the average value was obtained.