158532-72-0Relevant articles and documents
Synthesis and antiviral activity of C-5 substituted analogues of d4T bearing methylamino- or methyldiamino-linker arms
Gavriliu,Fossey,Fontaine,Benzaria,Ciurea,Delbederi,Lelong,Laduree,Aubertin,Kirn
, p. 1017 - 1031 (2000)
A general strategy is reported for the preparation of C-5-methylamino- or methyldiamino-d4t analogues of 'different sizes'. Reactions of the 2',3'- didehydro-2',3'-dideoxy-C-5 hydroxymethyl precursor (7) with either polymethylene diamines (n = 6, 8, 10 and 12) or propargylamine proceed regioselectively via substitution reactions at the C-5 position of uracil. The compounds were evaluated for antiviral activity and cytotoxicity. No significant activity was observed for compounds 9, 11, and 13, but 10 and 12 exhibited a weak activity against HIV-1.