Table 2. SAR of Substituent Effects of Styryl Group.
| LXRs
transactivation |
|||||||
|---|---|---|---|---|---|---|---|
| LXRs transrepression | agonistic
activity EC50 (μM) |
antagonistic
activity IC50 (μM)d |
|||||
| compd | bonda | R | % inhibition of IL-6 level at 10 μM | LXRα | LXRβ | LXRα | LXRβ |
| 7 | s | H | 31 | N.A.c | N.A.c | 13 | >30 (46%) |
| 20b | s | MeO | 35 | N.A.c | N.A.c | >30 (30%) | N.A.c |
| 17a | d | H | 12 | N.A.c | N.A.c | >30 (40%) | >30 (38%) |
| 17b | d | MeO | 50 | N.A.c | N.A.c | >30 (30%) | >30 (21%) |
| 17c | d | F | N.A.b | N.A.c | N.A.c | >30 (48%) | >30 (37%) |
| 17d | d | Br | 14 | N.A.c | N.A.c | >30 (21%) | >30 (28%) |
| 17e | d | CN | 27 | N.A.c | N.A.c | 27 | >30 (35%) |
| 17f | d | Me | 16 | N.A.c | N.A.c | >30 (49%) | >30 (20%) |
| 17g | d | CF3 | 27 | N.A.c | N.A.c | 23 | >30 (17%) |
| 17h | d | n-Bu | 29 | N.A.c | N.A.c | >30 (38%) | >30 (15%) |
| 17i | d | t-Bu | 16 | N.A.c | N.A.c | 6.8 | 6.8 |
a
s, single bond; d, double bond.
b
No activity at 10 μM.
c
No activity at 30 μM.
d
Percent inhibition at 30 μM is given in parentheses.