对映体2'，3'-双脱氧胞苷衍生物在细胞培养物中是有效的人类免疫缺陷病毒抑制剂。
Enantiomeric 2',3'-dideoxycytidine derivatives are potent human immunodeficiency virus inhibitors in cell cultures.
作者信息
Gosselin G, Mathé C, Bergogne M C, Aubertin A M, Kirn A, Schinazi R F, Sommadossi J P, Imbach J L
机构信息
Laboratoire de Chimie Bioorganique, URA CNRS 488, Université de Montpellier-II, Sciences et Techniques du Languedoc, Montpellier, France.
出版信息
C R Acad Sci III. 1994 Jan;317(1):85-9.
2',3'-dideoxy-beta-L-cytidine (beta-L-DDC) and its 5-fluoro derivative (beta-L-5-F-DDC) have been stereospecifically synthesized by a multi-step reaction sequence from L-xylose and their anti-HIV properties examined. Among these two L-enantiomers, the hitherto unknown beta-L-5-F-DDC emerged as a potent anti-HIV-1 and HIV-2 compound in different cell culture systems, with selectivity indices similar or superior to those of the currently licensed drug DDC which has the natural beta-D configuration.
已通过从L-木糖开始的多步反应序列立体定向合成了2',3'-二脱氧-β-L-胞苷（β-L-DDC）及其5-氟衍生物（β-L-5-F-DDC），并检测了它们的抗HIV特性。在这两种L-对映体中，迄今未知的β-L-5-F-DDC在不同细胞培养系统中成为一种有效的抗HIV-1和HIV-2化合物，其选择性指数与目前已获许可的具有天然β-D构型的药物DDC相似或更高。
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