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. 2019 Jun 5;24(11):2121. doi: 10.3390/molecules24112121

Table 1.

Cytotoxic effect of neocryptolepine derivatives [13,14,15,16].

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