Table 4.
Values of experimental and calculated data for DNA-duplexes stabilization and antitumor activity of acridinones
| Compound | ΔT m exp.a | ΔT m calc. | Δb | ILS exp.c | ILS calc. | Δ |
|---|---|---|---|---|---|---|
| C-1310 | 15.3 | 12.6 | 2.7 | 185 | 172 | 13 |
| C-1311 | 13.7 | 13.6 | 0.1 | 93 | 90 | 3 |
| C-1330 | 11.5 | 12.1 | 0.6 | 96 | 89 | 7 |
| C-1415 | 7.2 | 8.8 | 1.6 | 55 | 53 | 2 |
| C-1419 | 8.3 | 8.7 | 0.4 | 27 | 43 | 16 |
| C-1558 | 2.4 | 2.8 | 0.4 | 0 | 5 | 5 |
| C-1176 | 9.5 | 8.9 | 0.6 | 90 | 46 | 44 |
| C-1263 | 12.3 | 12.5 | 0.2 | 110 | 110 | 0 |
| C-1212 | 11.5 | 10.2 | 1.3 | 25 | 70 | 45 |
| C-1371 | 3.5 | 8.5 | 5.0 | 120 | 113 | 7 |
| C-1554 | 10.5 | 11.1 | 0.6 | 20 | 47 | 27 |
| C-1266 | 9.9 | 10.7 | 0.8 | 10 | −2 | 8 |
| C-1492 | 13.1 | 13.5 | 0.4 | 85 | 82 | 3 |
| C-1233 | 9.1 | 10.0 | 0.9 | 77 | 88 | 11 |
| C-1303 | 13.1 | 10.1 | 3.0 | 102 | 83 | 19 |
| C-1533 | 8.1 | 5.7 | 2.4 | 10 | 23 | 13 |
| C-1567 | 6.8 | 6.3 | 0.5 | 0 | 3 | 3 |
| C-1410 | 7.1 | 7.3 | 0.2 | 78 | 84 | 6 |
| C-1296 | 11.5 | 14.0 | 2.5 | 18 | −3 | 15 |
| C-1305 | 15.1 | 12.3 | 2.8 | 165 | 170 | 5 |
| Mean value of Δ | 1.4 | 13 | ||||
aThe increase in DNA melting temperature (expressed in centigrade degrees) at drug to DNA base pairs 0.25 M ratio
bDifference between experimental and calculated values
cThe percentage of increase in survival time of treated to control mice with P388 leukemia at optimal dose