Table 2.
Anti-proliferative Activities of compounds 69–74, 76–79, 81, 83, 85, 86.
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Entry | X | R | SKBr3 (IC50, μ M) | MCF-7 (IC50, μ M) | PC3 MM2 (IC50, μ M) | LNCap (IC50, μ M) | 253JB-V (IC50, μ M) |
69 | CH | H | 38.1±2.2 | 25.7±3.7 | NT | NT | NT |
70 | N | OH | 56.8±10.1 | 11.87±0.72 | NT | NT | NT |
71 | N | OCH2CH3 | 13.5±1.13 | 13.8±0.82 | 6.05±1.9 | 4.71±2.4 | NT |
72 | N | OCH2(CH2)2CH3 | 8.174±0.22 | 11.27±0.53 | 5.487±1.1 | 3.768±0.2 | NT |
73 | N | OCH2CH2Ph | >100 | 77.41±5.4 | 29.76±2.5 | 22.52±8.9 | NT |
74 | N | H | 9.1±0.12 | 10.30±0.17 | NT | NT | NT |
76 | N | O-a | 1.13±0.02 | 2.09±0.31 | 3.95±0.04 | 1.798±0.0 | NT |
77 | N | O-d | 0.21±0.04 | 0.41±0.04 | 0.68±0.2 | 0.40±0.19 | NT |
78 | N | O-f | 1.02±0.21 | 1.41±0.03 | 1.41±0.01 | 1.67±0.07 | 1.12±0.40 |
79 | N | O-cyclohexyl | 26.40±4.2 | 44.14±2.7 | 14.12±1.3 | 13.20±0.0 | 7.42±0.1 |
81 | N | O-g | 0.54±0.24 | 0.72±0.41 | 1.78±0.4 | 1.88±0.16 | 1.79±0.07 |
83 | N | O-b | 4.58±0.34 | 5.45±1.1 | 2.08±0.2 | 5.49±5.6 | 0.73±0.7 |
85 | N | O-c | 0.12±0.04 | 0.56±0.12 | 1.33±0.36 | 1.26±0.07 | 0.99±0.01 |
86 | N | O-h | 0.56±0.21 | 1.21±0.39 | 1.54±0.31 | 2.39±0.77 | 1.89±0.09 |