Table 2.
Antitumor and Cytotoxicity Activity of Diazapodophyllotoxin Analogues 69–73
Compds | Antitumor activity against P-388 leukemia T/C (%) @ different doses (mg/kg/injection)a | Cytotoxicity L1210 IC50 (μg/mL) | ||||||
---|---|---|---|---|---|---|---|---|
2.5 | 5 | 10 | 25 | 50 | 100 | 250 | ||
1 | 111 | 109 | 111 | <85 | 0.0036 | |||
69a | 117 | 144 | 161 | 239 | 0.42 | |||
69b | 123 | 137 | 159 | 214 | 0.22 | |||
69c | 119 | 131 | 153 | 165 | 233 | <85 | 0.052 | |
69d | 117 | 133 | 150 | 172 | 94 | <85 | 0.080 | |
70a | 111 | 124 | 128 | 150 | 161 | 172 | >326 | 0.050 |
70b | 110 | 139 | 156 | 206 | 206 | 0.16 | ||
70c | 139 | 144 | 156 | 177 | <85 | 0.055 | ||
70d | 114 | 131 | 147 | 199 | <85 | 0.028 | ||
71 | 111 | 122 | 147 | 147 | 161 | 0.75 | ||
72 | 104 | 109 | 114 | 134 | 153 | <85 | 0.090 | |
73 | 104 | 109 | 109 | 111 | 109 | 144 | 0.54 |
single i.p. treatment on day 1. T/C, median survival time of test animals/median survival time of control animals; 125% or above considered active; <85% considered toxic.