Synthesis and Anti-HIV-1 Activity of Base Modified Analogues of 3′-Azido-2′,3′-Dideoxythymidine (AZT)

Analogues of AZT have been synthesized by modifications at the 4-position of the base. Two synthetic routes are described. Among the new compounds, 3′-azido-2′, 3′-dideoxy-4-thiouridine 2b exhibited an unexpectedly marked anti-HIV activity on CEM-C113 cell lines.