Table 1.
Antiproliferation effect of the selected compound on LNCaP95 and 22RV1 cell lines.
| |||||
|---|---|---|---|---|---|
| Compounds | Structure | Inhibitory Rate | IC50 (μM) a | ||
| R1 | R2 | 22RV1 @1.0 μM | LNCaP95 | 22RV1 | |
| DMSO | −2.10% | Nt b | Nt b | ||
| A1 | 4-Cl | 2′-F | 54.3% | 1.19 ± 0.53 | 0.467 ± 0.131 |
| A2 | 2′-CH3 | 47.1% | 0.620 ± 0.311 | 0.676 ± 0.245 | |
| A3 | 2′-OCH3 | 50.0% | 2.48 ± 0.702 | 0.714 ± 0.303 | |
| A4 | 3′-Cl | 47.5% | 3.43 ± 0.49 | 0.713 ± 0.178 | |
| A5 | 3′-F | 44.2% | 0.937 ± 0.351 | 0.924 ± 0.414 | |
| A6 | 3′-CF3 | 54.4% | 0.214 ± 0.067 | 0.424 ± 0.120 | |
| A7 | 3′-CH3 | 42.5% | 0.789 ± 0.436 | 0.976 ± 0.205 | |
| A8 | 3′-OCH3 | 35.9% | 0.615 ± 0.138 | 2.11 ± 0.52 | |
| A9 | 5-Cl | H | 44.9% | 0.812 ± 0.374 | 0.581 ± 0.289 |
| A10 | 2′-F | 56.0% | 0.373 ± 0.069 | 0.271 ± 0.125 | |
| A11 | 2′-CF3 | −8.30% | nt b | Nt b | |
| A12 | 2′-CH3 | 58.0% | 0.493 ± 0.105 | 0.248 ± 0.063 | |
| A13 | 2′-OCH3 | 57.3% | 0.444 ± 0.119 | 0.158 ± 0.044 | |
| A14 | 3′-Cl | 51.3% | 1.67 ± 0.25 | 0.386 ± 0.171 | |
| A15 | 3′-F | 55.4% | 0.755 ± 0.221 | 0.280 ± 0.092 | |
| A16 | 3′-CF3 | 47.5% | 0.693 ± 0.314 | 0.556 ± 0.112 | |
| A17 | 3′-CH3 | 50.1% | 0.867 ± 0.298 | 0.324 ± 0.058 | |
| A18 | 3′-OCH3 | 55.4% | 2.11 ± 0.46 | 0.483 ± 0.145 | |
| A19 | 5-Br | 2′-Cl | 13.40% | Nt b | nt b |
| A20 | 2′-OCH3 | 60.2% | 0.304 ± 0.053 | 0.242 ± 0.044 | |
| B1 | 5-Cl | 3′, 4′-diCF3 | 59.2% | 0.239 ± 0.072 | 0.258 ± 0.097 |
| B2 | 2′-Cl, 4′-NH2 | 19.60% | nt b | nt b | |
| B3 | 3′-CF3, 4′-CN | 34.9% | 0.354 ± 0.066 | 0.695 ± 0.246 | |
| B4 | 5-Br | 3′, 4′-diCF3 | 53.1% | 0.213 ± 0.042 | 0.307 ± 0.059 |
| B5 | 5-F | 2′-Cl, 4′-CF3 | 59.2% | 0.384 ± 0.088 | 0.375 ± 0.063 |
| B6 | 2′-F, 4′-CF3 | 62.5% | 0.185 ± 0.041 | 0.196 ± 0.032 | |
| B7 | 2′-CN, 4′-CF3 | 42.3% | 4.38 ± 1.33 | 7.92 ± 2.56 | |
| B8 | 3′-CN, 4′-CF3 | 60.4% | 0.396 ± 0.065 | 0.240 ± 0.048 | |
| B9 | 3′, 4′-diCF3 | 84.3% | 0.130 ± 0.033 | 0.0997 ± 0.0221 | |
| B10 |
|
42.3% | 0.627 ± 0.225 | 0.547 ± 0.153 | |
| B11 |
|
47.7% | 0.392 ± 0.136 | 0.581 ± 0.205 | |
| B12 | 2′-Cl, 4′-CN | 44.3% | 14.0 ± 5.6 | 3.23 ± 1.84 | |
| B13 | 2′-F, 4′-CN | 65.6% | 0.231 ± 0.072 | 0.184 ± 0.061 | |
| B14 | 4,5-diF | 3′, 4′-diCF3 | 47.3% | 0.199 ± 0.055 | 0.382 ± 0.078 |
| B15 | 5-CN | 44.8% | 2.35 ± 0.53 | 1.04 ± 0.26 | |
| B16 | 5-CF3 | 64.6% | 0.113 ± 0.044 | 0.111 ± 0.023 | |
| C1 | 5-Cl | 3′, 4′-diCF3 | 53.1% | 0.299± | 0.320 ± 0.115 |
|
C2
C3 |
2′-Cl, 4′-NO2 | 19.0% | nt b | nt b | |
| 3′-CF3, 4′-NO2 | 43.7% | 0.330 ± 0.081 | 0.557 ± 0.127 | ||
| C4 | 5-Br | 2′-Cl, 4′-NO2 | 31.2% | nt b | nt b |
| C5 | 3′-CF3, 4′-NO2 | 58.3% | 0.536 ± 0.201 | 0.306 ± 0.058 | |
| C6 | 2-TfO, 4-Cl | 3′-CH3, 4′-NO2 | 59.4% | 0.485 ± 0.147 | 0.268 ± 0.066 |
| C7 | 2-AcO, 5-Cl | 2′-Cl, 4′-NO2 | 42.9% | 0.386 ± 0.098 | 0.481 ± 0.113 |
| C8 | 2-TfO, 5-Cl | 59.2% | 0.196 ± 0.064 | 0.252 ± 0.092 | |
| Niclosamide | 55.8% | 0.372 ± 0.074 | 0.284 ± 0.059 | ||
| Enzalutamide | 24.1% | >10,000 | 695 | ||
a The data given are means of three independent experiments. b nt = not tested.