某些具有不同功能化的螺环丙基衍生物对人类免疫缺陷病毒1型（HIV-1）复制的抑制作用。

Inhibition of human immunodeficiency virus type (HIV-1) replication by some diversely functionalized spirocyclopropyl derivatives.

作者信息

Witvrouw M, Pannecouque C, De Clercq E, Fernández-Alvarez E, Marco J L

机构信息

Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium.

出版信息

Arch Pharm (Weinheim). 1999 May;332(5):163-6. doi: 10.1002/(sici)1521-4184(19995)332:5<163::aid-ardp163>3.0.co;2-2.

DOI:10.1002/(sici)1521-4184(19995)332:5<163::aid-ardp163>3.0.co;2-2

PMID:10366901

Abstract

Inhibition of HIV-1 replication by differently substituted spirocyclopropyl compounds has been evaluated. Compound 21 showed a moderate activity (EC50 ranging from 2.3 to 5.8 micrograms/ml) against different HIV-1 strains (IIIB, RF, NDK, and an AZT-resistant strain) in different cell lines (MT-4 and C-8166 cells), while it was cytotoxic at 77.7 micrograms/ml, resulting in a selectivity index of 34. This compound was inactive against HIV-2 (ROD) and SIV (MAC251). From "time-of-addition" experiments compound 21, like AZT, appeared to inhibit HIV-1 at the reverse transcriptase step.

摘要

已评估了不同取代的螺环丙基化合物对HIV-1复制的抑制作用。化合物21在不同细胞系（MT-4和C-8166细胞）中对不同HIV-1毒株（IIIB、RF、NDK和一株齐多夫定耐药毒株）表现出中等活性（EC50为2.3至5.8微克/毫升），而其细胞毒性为77.7微克/毫升，选择性指数为34。该化合物对HIV-2（ROD）和猴免疫缺陷病毒（SIV，MAC251）无活性。从“添加时间”实验来看，化合物21与齐多夫定一样，似乎在逆转录酶步骤抑制HIV-1。