Table 1.
No. | Substituent | IC50 μM | |||||||
---|---|---|---|---|---|---|---|---|---|
R1 | R2 | R3 | R4 | R5 | BALB/3T3 | MV4-11 | A549 | HCT116 | |
7a | H | NH(CH2)3NH2 | H | Me | - | 0.884 ± 0.115 | 0.066 ± 0.023 | 0.205 ± 0.079 | 0.302 ± 0.056 |
7b | Cl | NH(CH2)3NH2 | H | Me | - | 0.401 ± 0.015 | 0.068 ± 0.018 | 0.761 ± 0.169 | 0.195 ± 0.044 |
7c | Br | NH(CH2)3NH2 | H | Me | - | 0.869 ± 0.018 | 0.012 ± 0.002 | 0.543 ± 0.256 | 0.274 ± 0.050 |
7d | OMe | NH(CH2)3NH2 | H | Me | - | 0.978 ± 0.021 | 0.102 ± 0.021 | 0.407 ± 0.117 | 0.155 ± 0.042 |
7e | Cl | NHCH2CH(OH)CH2NH2 | H | Me | - | 0.896 ± 0.042 | 0.042 ± 0.014 | 0.197 ± 0.028 | 0.138 ± 0.050 |
7f | Br | NHCH2CH(OH)CH2NH2 | H | Me | - | 0.864 ± 0.015 | 0.057 ± 0.015 | 0.190 ± 0.027 | 0.117 ± 0.055 |
7g | H | NH(CH2)3NH2 | COOMe | Me | - | 0.933 ± 0.047 | 0.044 ± 0.011 | 0.820 ± 0.456 | 0.176 ± 0.055 |
7h | Br | NH(CH2)3NH2 | COOMe | Me | - | 0.773 ± 0.023 | 0.050 ± 0.016 | 0.302 ± 0.138 | 0.164 ± 0.070 |
7i | Cl | NH(CH2)3NH2 | COOMe | Me | - | 0.833 ± 0.030 | 0.056 ± 0.035 | 0.194 ± 0.063 | 0.116 ± 0.078 |
7j | Cl | NH(CH2)3NH2 | Br | Me | - | 0.834 ± 0.067 | 0.076 ± 0.034 | 0.464 ± 0.011 | 0.284 ± 0.142 |
8 | Cl | NH(CH2)2NH2 | H | - | Me | 0.437 ± 0.400 | 0.456 ± 0.123 | 8.282 ± 0.585 | 6.989 ± 1.416 |
9 | OMe | NH(CH2)2NH2 | H | - | - | 6.87 ± 1.74 | 0.12 ± 0.07 | 9.29 ± 1.10 | 1.93 ± 0.24 |
Cisplatin | 8.53 ± 3.53 | 2.36 ± 0.68 | 7.83 ± 2.60 | 3.47 ± 0.77 | |||||
Doxorubicin HCl | 1.08 ± 0.03 | 0.006 ± 0.002 | 0.33 ± 0.10 | 0.39 ± 0.10 |