| Compound |
EC50(mM)a) |
CC50(mM) |
S.I |
| 4’-C-cyanothymidine |
0.002 |
1 |
500 |
| 4’-C-azidothymidine |
0.01 |
8 |
300 |
| 4’-C-ethynylthymidine |
0.83 |
>400 |
>482 |
| 4’-C-ethynylarabinofuranosylthymidine |
119 |
>400 |
>3.4 |
| 4’-C-azidomethylthymidine |
2.1 |
333 |
159 |
| 4’-C-methylthymidine |
7.2 |
104 |
14 |
| 4’-C-ethylthymidine |
>400 |
400 |
ND |
| 4’-C-methoxythymidine |
8.49 |
200 |
24 |
| 4’-C-vinylthymidine |
>400 |
>400 |
ND |
| 4’-C-hydroxymethylthymidine |
7.0 |
>400 |
>57 |
| 4’-C-propylthymidine |
>100 |
>100 |
ND |
| 4’-C-cyano-2’-deoxycytidine |
0.0012 |
0.17 |
142 |
| 4’-C-azido-2’-deoxycytidine |
0.004 |
0.21 |
52 |
| 4’-C-ethyny-2’-deoxycytidine |
0.0048 |
2.2 |
458 |
| L-4’-C-ethynyl-2’-deoxycytidine |
>400 |
>400 |
ND |
| 4’-C-ethynyl-2’-deoxy-5-fluorocytidine |
0.030 |
>100 |
>3333 |
| 4’-C-ethynylarabinofuranosylcytidine |
0.043 |
2.0 |
46.5 |
| 4’-C-methyl-2’-deoxycytidine |
0.015 |
1.0 |
66.7 |
| 4’-C-fluoromethyl-2’-deoxycytidine |
0.0068 |
0.12 |
18 |
| 4’-C-methyl-2’-deoxyadenosine |
2.6 |
2.6 |
1 |
| 4’-C-azido-2’-deoxyadenosine |
0.13 |
50 |
385 |
| 4’-C-ethyny-2’-deoxyadenosine |
0.098 |
16 |
1630 |
| 2’,3’-dideoxy-3’-thia-L-cyrtidine (3TC) |
0.10 |
>100 |
>1000 |
| 3’-azido-3’-deoxythymidine (AZT) |
0.0032 |
29.4 |
9190 |
a) Anti-HIV activity was determined by MTT assay. MT-4 cells and HIV-1