Entry | R1 | R2 | R | R′ | IC50 ± SD (µM)a |  | ||
---|---|---|---|---|---|---|---|---|
MCF-7 | SW480 | A-549 | NIH/3T3 | |||||
7a | Cl | Cl | H | hydrazine |  > 200 |  > 200 |  > 200 | ND |
7b | Cl | Cl | 4-F | hydrazine |  > 200 | 52.05 ± 4.17 | 80.05 ± 9.89 | 73.70 ± 2.40 |
7c | Cl | Cl | 4-Cl | hydrazine |  > 200 |  > 200 | 25.85 ± 1.20 | 48.55 ± 8.41 |
7d | Cl | Cl | H | hydroxyurea |  > 200 |  > 200 | 45.10 ± 1.97 | ND |
7e | Cl | Cl | 4-Cl | hydroxyurea |  > 200 |  > 200 |  > 200 | ND |
7f | Cl | Cl | H | dimethylurea |  > 200 |  > 200 |  > 200 | 38.25 ± 3.18 |
7g | Cl | Cl | H | p-tolylhydrazine |  > 200 | 131.90 ± 5.09 |  > 200 | ND |
7h | Cl | Cl | H | (3-chlorophenyl) hydrazine |  > 200 |  > 200 |  > 200 | ND |
7i | Br | H | H | hydrazine | 46.35 ± 4.03 | 136.25 ± 1.76 | 53.5 ± 0.70 | 102.5 ± 7.07 |
7j | Br | H | 4-F | hydrazine | 10.01 ± 5.5 | 14.65 ± 5.44 | 63.85 ± 6.57 |  > 200 |
7k | Br | H | 4-Cl | hydrazine | 12.84 ± 0.84 | 10.90 ± 0.84 | 79.25 ± 5.30 | 19.70 ± 8.06 |
7l | Br | H | H | hydroxyurea | 29.60 ± 2.26 |  > 200 | 28.00 ± 9.89 | 121.65 ± 11.52 |
7m | Br | H | H | dimethylurea | 108.75 ± 5.30 |  > 200 | 31.08 ± 3.25 | ND |
7n | Br | H | H | p-tolylhydrazine |  > 200 | 85.35 ± 0.63 | 17.40 ± 1.41 | 14.85 ± 1.90 |
7o | Br | H | 4-Cl | (3-chlorophenyl) hydrazine | 165.65 ± 6.85 | 69.50 ± 7.77 |  > 200 | 26.75 ± 0.35 |
Cisplatin | – | – | – | – | 9.90 ± 0.27 | 15.25 ± 1.1 | – | – |
Erlotinib | – | – | – | – | 39.30 ± 1.13 | 11.18 ± 0.38 | – | – |