Table 2.
The cell viability of the target compounds on MCF-7, T-47D, T-47DY537S and T-47DD538G cell lines (IC50, μmol/L)a.
| Entry | Compd. | R1 | R2 | R3 | MCF-7 (μmol/L) | T-47D (μmol/L) | T-47DD538G (μmol/L) | T-47DY537S (μmol/L) |
|---|---|---|---|---|---|---|---|---|
| 1 | 26a |  |
/ | / | 7.72 ± 0.64 | >31 | >31 | 27.22 ± 0.73 |
| 2 | 26b |  |
/ | / | 9.18 ± 0.95 | 19.38 ± 0.54 | >31 | >31 |
| 3 | 26c |  |
/ | / | 3.16 ± 0.63 | 15.84 ± 0.68 | 8.75 ± 0.25 | 12.02 ± 0.40 |
| 4 | 26d |  |
/ | / | 1.79 ± 0.40 | 6.91 ± 0.29 | 9.33 ± 0.46 | 8.93 ± 0.25 |
| 5 | 26e |  |
/ | / | 3.42 ± 0.32 | 8.20 ± 0.36 | 7.86 ± 0.37 | 8.85 ± 0.61 |
| 6 | 26f |  |
/ | / | 0.50 ± 0.30 | 9.11 ± 0.21 | >31 | >31 |
| 7b | 28a |  |
/ | / | 5.07 ± 0.71 | >31 | >31 | >31 |
| 8b | 28b | |
/ | / | 0.44 ± 0.11 | 25.58 ± 0.98 | 17.13 ± 0.65 | >31 |
| 9b | 28c | |
/ | / | 0.35 ± 0.02 | 24.92 ± 0.77 | 17.63 ± 0.89 | >31 |
| 10b | 28d | |
/ | / | 0.66 ± 0.12 | 13.35 ± 0.77 | >31 | >31 |
| 11b | 28e | |
/ | / | 1.10 ± 0.14 | 19.72 ± 0.32 | >31 | >31 |
| 12b | 28f | |
4-OH | / | 0.93 ± 0.19 | 8.53 ± 0.12 | >31 | 9.11 ± 0.35 |
| 13 | 29a | |
4-OH | CF3 | 0.18 ± 0.05 | 2.85 ± 0.29 | 5.55 ± 0.24 | >31 |
| 14 | 29b | |
4-OH | CF3 | 0.36 ± 0.04 | 5.12 ± 0.33 | >31 | >31 |
| 15 | 29c | |
4-OH | CF3 | 0.056 ± 0.004 | 0.87 ± 0.15 | 1.91 ± 0.18 | 0.88 ± 0.15 |
| 16c | 29c′ | |
4-OH | CF3 | 0.95 ± 0.11 | 5.52 ± 0.27 | 5.00 ± 0.36 | 4.05 ± 0.27 |
| 17 | 29d | |
4-Me | CF3 | 0.75 ± 0.21 | 8.33 ± 0.22 | >31 | >31 |
| 18 | 29e | |
H | CF3 | 0.66 ± 0.12 | 5.10 ± 0.32 | 5.18 ± 0.31 | 1.79 ± 0.17 |
| 19 | 29f | |
4-OMe | CF3 | 0.094 ± 0.001 | 8.58 ± 0.36 | 8.53 ± 0.47 | >31 |
| 20 | 29g | |
4-F | CF3 | 0.64 ± 0.10 | 5.28 ± 0.23 | 7.82 ± 0.47 | >31 |
| 21 | 29h | |
3-OH | CF3 | 0.98 ± 0.35 | 3.92 ± 0.01 | 2.84 ± 0.14 | 2.99 ± 0.22 |
| 22 | 29i | |
4-OH | CH3 | 0.071 ± 0.027 | 3.49 ± 0.06 | 4.25 ± 0.19 | 1.89 ± 0.17 |
| 23 | 29j | |
4-OMe | CH3 | 0.29 ± 0.03 | 7.92 ± 0.19 | 8.25 ± 0.45 | 12.72 ± 0.53 |
| 24 | 29k |  |
4-OH | CF3 | 1.06 ± 0.19 | >31 | >31 | >31 |
| 25 | 29l | NH2 | 4-OH | CF3 | 3.17 ± 0.33 | 8.11 ± 0.37 | >31 | >31 |
| 26 | 29m | OH |  |
CF3 | 0.16 ± 0.04 | 7.66 ± 0.60 | 3.68 ± 0.39 | 3.31 ± 0.34 |
| 27d | 6a | 0.25 ± 0.10 | >31 | >31 | >31 | |||
| 28 | 4-OHT | 0.67 ± 0.08 | 1.95 ± 0.20 | 9.13 ± 0.60 | 8.90 ± 0.28 | |||
| 29 | Ful | 0.14 ± 0.05 | 1.76 ± 0.06 | 3.92 ± 0.22 | 2.22 ± 0.17 |
a
Values are the mean ± SD of at least three parallel tests.
b
Series II compounds were mixtures of regioisomers.
c
Compound 29c′ was regioisomer of 29c.
d
6a was a derivative of OBHSA, X = NCH2CF3, R = 4-OH.