Baba M, Pauwels R, Herdewijn P, De Clercq E, Desmyter J, Vandeputte M
Biochem Biophys Res Commun. 1987 Jan 15;142(1):128-34. doi: 10.1016/0006-291x(87)90460-8.
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 microM and 0.04 microM, 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 microM and 0.04 microM, respectively. Their selectivity indexes, as based on the ratio of the 50% cytotoxic dose to the 50% antiviral effective dose, were 120 (ddeThd) and greater than 625 (ddThd).
2',3'-双脱氧胸苷（ddThd）及其2',3'-不饱和衍生物2',3'-双脱氧胸苷烯（ddeThd）在体外是人类免疫缺陷病毒（HIV）的强效和选择性抑制剂。当评估它们对MT-4细胞中HIV细胞病变效应的抑制作用时，ddThd和ddeThd分别在浓度为1微摩尔和0.04微摩尔时完全保护细胞免受病毒破坏。在这方面，ddeThd的效力约为2',3'-双脱氧胞苷（ddCyd）的5倍，ddCyd是目前因其在治疗艾滋病方面的治疗潜力而被研究的最有效的选择性抗HIV化合物之一。ddThd和ddeThd也分别在1微摩尔和0.04微摩尔时抑制HIV抗原表达。基于50%细胞毒性剂量与50%抗病毒有效剂量之比的选择性指数分别为120（ddeThd）和大于625（ddThd）。
