Table 3. Cytotoxic Activity of 3′-dA and Compounds 7a,b, d–fa.
| HEL92.1.7 |
NCI-H929 |
RPMI-8226 |
Jurkat |
Z138 |
RL |
HS445 |
||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| comp | LC50 | MI% | LC50 | MI% | LC50 | MI% | LC50 | MI% | LC50 | MI% | LC50 | MI% | LC50 | MI% |
| 3′-dA | 68.9 | 88 | >198 | 24 | >198 | 1 | >198 | 20 | 12.15 | 95 | >198 | 17 | >198 | 2 |
| 7a | 8.07 | 100 | 6.07 | 100 | 14.72 | 96 | 1.44 | 100 | 26.97 | 95 | 3 | 93 | 30.53 | 98 |
| Rp-7a | 11.0 | 98 | 19.0 | 97 | 25.0 | 90.8 | 2.82 | 97 | - | - | 4.0 | 96.8 | 42.0 | 99 |
| Sp-7a | 11.0 | 100 | 16.0 | 94 | 19.0 | 86.8 | 2.29 | 90 | - | - | 2.64 | 92.6 | 67.0 | 75 |
| 7b | 2.94 | 98 | 3.38 | 99 | 9.48 | 102 | 0.9 | 100 | 6.32 | 100 | 1.68 | 96 | 10.18 | 96 |
| 7d | 4.23 | 99 | 7.21 | 104 | 24.06 | 103 | 7.15 | 100 | 5.65 | 100 | 11.61 | 100 | 39.53 | 102 |
| 7e | 14.49 | 99 | 7.57 | 100 | 31.05 | 106 | 4.75 | 100 | 68.18 | 76 | 7.26 | 90 | 42.73 | 92 |
| 7f | 15.42 | 101 | 16.11 | 98 | 46.7 | 89 | 7.01 | 95 | 43.84 | 93 | 13.54 | 88 | 54.98 | 85 |
| PTX | 0.02 | 83 | 0.003 | 82 | 0.003 | 91 | 0.005 | 97 | 0.002 | 99 | 0.003 | 83 | 0.01 | 74 |
Cytotoxicity data reported as μM LC50 values (concentration of drug causing 50% cell death) and MI% values (maximum inhibitory effect of the drug at the range of concentrations considered). PTX: paclitaxel (control); (-) not tested.