Both 2′,3′-dideoxythymidine and its 2′,3′-unsaturated derivative (2′,3′-dideoxythymidinene) are potent and selective inhibitors of human immunodeficiency virus replication in vitro

doi:10.1016/0006-291X(87)90460-8

Biochemical and Biophysical Research Communications

Volume 142, Issue 1, 15 January 1987, Pages 128-134

https://doi.org/10.1016/0006-291X(87)90460-8 Get rights and content

Abstract

2′,3′-Dideoxythymidine (ddThd) and its 2′,3′-unsaturated derivative 2′,3′-dideoxythymidinene (ddeThd) are potent and selective inhibitors of human immunodeficiency virus (HIV) in vitro. When evaluated for their inhibitory effects on the cytopathogenicity of HIV in MT-4 cells, ddThd and ddeThd completely protected the cells against destruction by the virus at a concentration of 1 μM and 0.04 μM, respectively. In this aspect, ddeThd was about 5 times more potent than 2′,3′-dideoxycytidine (ddCyd), one of the most potent and selective anti-HIV compounds now pursued for its therapeutic potential in the treatment of AIDS. ddThd and ddeThd also suppressed HIV antigen expression at 1 μM and 0.04 μM, respectively. Their selectivity indexes, as based on the ratio of the 50 % cytotoxic dose to the 50 % antiviral effective dose, were 120 (ddeThd) and > 625 (ddThd).

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Both 2′,3′-dideoxythymidine and its 2′,3′-unsaturated derivative (2′,3′-dideoxythymidinene) are potent and selective inhibitors of human immunodeficiency virus replication in vitro

Abstract

Lancet

Biochem. Biophys. Res. Commun

Science

New Engl. J. Med

Science