Table 3. Modification in the Lipophilic Tail Region1.
| no. | R2 | RXRα EC50 [μM] | RXRβ EC50 [μM] | RXRγ EC50 [μM] |
|---|---|---|---|---|
| 14 | Ph | >30 | >30 | >30 |
| 15 | 4-Cl-Ph | >30 | >30 | >30 |
| 16 | 4-Br-Ph | 40 ± 4 (21 ± 4%) | 48 ± 10 (36 ± 15%) | >30 |
| 17 | 4-I-Ph | 24 ± 1 (19 ± 1%) | 29 ± 2 (25 ± 2%) | >30 |
| 18 | 4-Et-Ph | 28 ± 3 (11 ± 1%) | 35 ± 3 (7.4 ± 0.7%) | i.a. |
| 19 | 4-iPr-Ph | 16 ± 1 (11 ± 1%) | 16 ± 1 (9.5 ± 0.5%) | i.a. |
| 4 | 4-tBu-Ph | 7.8 ± 2.4 (16 ± 4%) | 8.9 ± 0.4 (15 ± 1%) | >30 |
| 20 | 3-Cl-Ph | 17 ± 1 (54 ± 3%) | 20 ± 4 (26 ± 5%) | 44 ± 16 (9.3 ± 3.4%) |
| 21 | 2-Cl-Ph | 9.9 ± 0.5 (58 ± 2%) | 8.3 ± 0.8 (31 ± 2%) | >30 |
| 22 | 2-F-Ph | >30 | >30 | >30 |
| 23 | 2-CH3-Ph | 5.0 ± 0.1 (24 ± 1%) | 8.6 ± 1.1 (27 ± 2%) | 19 ± 1 (19 ± 1%) |
| 24 | 2-CF3-Ph | 1.1 ± 0.1 (22 ± 1%) | 2.1 ± 0.1 (22 ± 1%) | 10 ± 1 (52 ± 1%) |
| 25 | 2-OCH3-Ph | 29 ± 1 (21 ± 1%) | >30 | >30 |
| 26 | 2-OCF3-Ph | 1.1 ± 0.1 (26 ± 1%) | 1.9 ± 0.1 (18 ± 1%) | 4.2 ± 0.1 (25 ± 1%) |
| 27 | 2-tBu-Ph | 0.16 ± 0.01 (11 ± 1%) | 0.37 ± 0.03 (12 ± 1%) | 1.1 ± 0.1 (21 ± 1%) |
| 28 | (1,1′-biphenyl)-2-yl | 0.28 ± 0.01 (70 ± 1%) | 0.31 ± 0.01 (44 ± 1%) | 1.6 ± 0.1 (94 ± 4%) |
1
i.a., inactive at 30 μM; relative activation efficacy compared to 1 (1 μM) is shown in parentheses. All values are mean ± SEM; n ≥ 3.