Table 2. . Antiproliferative evaluation of compounds 130–178 against A549 and MCF7 cells†,‡,§,¶.
| ||||
|---|---|---|---|---|
| Compound | R1 | R2 | A549 IC50 (μM) | MCF7 IC50 (μM) |
| 130 | 4-Cl | 4-Cl | >50 | 17.2 (±0.9) |
| 131 | 4-Br | 4-Cl | 10.9 (±0.7) | 21.3 (±1.6) |
| 132 | 4-I | 4-Cl | 8.7 (±0.6) | 41.1 (±3.1) |
| 133 | 4-CN | 4-Cl | 41.1 (±3.8) | 18.8 (±1.6) |
| 134 | 4-NO2 | 4-Cl | >50 | 16.7 (±1.3) |
| 135 | 4-CF3 | 4-Cl | 19.5 (±0.8) | 14.7 (±0.7) |
| 136 | 4-CO2CH3 | 4-Cl | 26.3 (±1.1) | 13.7 (±1.2) |
| 137 | 4-CH3 | 4-Cl | 14.6 (±0.9) | 23.0 (±1.8) |
| 138 | 4-Ph | 4-Cl | 17.2 (±1.5) | 9.8 (±0.7) |
| 139 | 4-OCH3 | 4-Cl | 22.5 (±2.1) | 23.1 (±2.0) |
| 140 | 3-F | 4-Cl | 24.6 (±2.2) | 24.3 (±2.1) |
| 141 | 3-Cl | 4-Cl | 27.0 (±2.4) | 18.2 (±1.6) |
| 142 | 3-Br | 4-Cl | 13.1 (±1.2) | 15.8 (±1.2) |
| 143 | 3-CN | 4-Cl | 27.8 (±1.6) | 42.4 (±3.3) |
| 144 | 3-NO2 | 4-Cl | >50 | 19.3 (±1.5) |
| 145 | 3-CF3 | 4-Cl | 12.9 (±0.9) | 9.8 (±0.8) |
| 146 | 3-CO2CH3 | 4-Cl | 23.9 (±1.9) | 32.0 (±2.2) |
| 147 | 3-CH3 | 4-Cl | 16.4 (±1.1) | 26.0 (±2.1) |
| 148 | 3-Ph | 4-Cl | >50 | >50 |
| 149 | 3-OCH3 | 4-Cl | 7.6 (±0.7) | 21.0 (±1.2) |
| 150 | 2-Cl | 4-Cl | 20.2 (±1.5) | 23.2 (±1.9) |
| 151 | 2-I | 4-Cl | 36.3 (±3.3) | 26.2 (±1.9) |
| 152 | 2-CN | 4-Cl | 23.1 (±1.7) | 40.1 (±3.3) |
| 153 | 2-NO2 | 4-Cl | >50 | >50 |
| 154 | 2-CF3 | 4-Cl | 38.5 (±2.8) | 43.3 (±4.1) |
| 155 | 2-CH3 | 4-Cl | 28.0 (±2.6) | 19.1 (±1.8) |
| 156 | 4-Cl | 4-F | 21.2 (±1.6) | 8.2 (±0.7) |
| 157 | 4-Cl | 4-Br | 46.7 (±3.7) | 18.5 (±1.5) |
| 158 | 4-Cl | 4-I | 21.1 (±2.1) | 14.1 (±1.2) |
| 159 | 4-Cl | 4-CF3 | 22.2 (±2.1) | 12.4 (±1.3) |
| 160 | 4-Cl | 4-CH3 | 21.0 (±2.0) | 11.7 (±1.1) |
| 161 | 4-Cl | 4-Ph | >50 | 19.8 (±1.4) |
| 162 | 4-Cl | 4-OCH3 | 20.4 (±0.9) | 8.0 (±0.6) |
| 163 | 4-Cl | 3-F | 21.2 (±1.8) | 13.5 (±1.1) |
| 164 | 4-Cl | 3-Cl | 22.8 (±1.8) | 14.7 (±1.2) |
| 165 | 4-Cl | 3-Br | >50 | 18.5 (±1.7) |
| 166 | 4-Cl | 3-I | 40.5 (±3.4) | 21.6 (±1.7) |
| 167 | 4-Cl | 3-CN | >50 | 19.4 (±1.5) |
| 168 | 4-Cl | 3-CF3 | 20.2 (±1.9) | 10.5 (±1.0) |
| 169 | 4-Cl | 3-CH3 | 20.4 (±1.0) | 14.1 (±1.1) |
| 170 | 4-Cl | 3-Ph | >50 | >50 |
| 171 | 4-Cl | 3-OCH3 | 21.1 (±1.9) | 18.8 (±1.4) |
| 172 | 4-Cl | 2-F | >50 | 17.6 (±1.4) |
| 173 | 4-Cl | 2-Br | 25.0 (±2.0) | 6.9 (±0.5) |
| 174 | 4-Cl | 2-I | >50 | 32.9 (±2.4) |
| 175 | 4-Cl | 2-CF3 | 22.6 (±1.7) | >50 |
| 176 | 4-Cl | 2-CH3 | 19.2 (±1.9) | 7.4 (±0.6) |
| 177 | 4-Cl | 2-Ph | 23.3 (±1.8) | 18.3 (±1.3) |
| 178 | 4-Cl | 2-OCH3 | 34.3 (±2.6) | 5.8 (±0.7) |
†
A549 and MCF7 cells were incubated for 24 h prior to drug addition.
‡
A549 and MCF7 cells were incubated for 72 h at 37°C in 5% CO2 with the respective drug.
§
Cell proliferation was determined using an MTT assay.
¶
All experiments were performed in replicates of 6–8.