Structure Base EC50(μM) CC50(μM) SI(CC50/EC50)
4’MdN Ad
Th
Cy
Purine
2.6
7.2
0.072
1.9
2.6
104
0.13
>200
1.0
-
1.8
>100
4’Md4N Ad
Th
Cy
>500
21
350
>500
330
350
~1
16
-
4’MddN Ad
Th
Cy
30
>500
27
400
>500
27
13
~1
1
AZT
ddA
d4T
0.001
47
4.1
>20
>500
>500
>2020
>11
>120
EC50=50% effective concentration; CC50=Cytotoxic concentration; SI-Selectivitiy index (CC50/EC50); 4’MdN=4’=C-methyl-2’-deoxynucleoside; 4’Md4N=4’-C-methyl- 2’-3’-didehydrodi deoxynucleoside; 4’MddN=4’-C-methyl-2’-3’-dideoxy nucleoside; AZT=3’-azido-3’deoxythymidine; ddA=2’,3’-dideoxyadenosine; d4T=2’,3’- didehydro-3’-deoxythymidine
Table 1: Anti-HIV activety of 4’-C-methyl-2’-deoxynucleosides.
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