The enzymatic synthesis and ant HIV-1 activity of 9-beta-D-2 ',3 '-dideoxynucleosides of N(6)-substituted purines

被引:6
作者
Betbeder, D. [1 ]
Hutchinson, D. W. [1 ]
Richards, A. O'L [1 ]
Mahood, N. [2 ]
Kinchington, D. [3 ]
机构
[1] Warwick Univ, Chem Dept, Coventry CV4 7AL, W Midlands, England
[2] Med Res Council Collaborat Ctr, London NW7 1AD, England
[3] St Marys Hosp, Med Sch, Dept Med Microbiol, Div Virol, London WC2 1PG, England
关键词
D O I
10.1177/095632029000100404
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
9-beta-D-2',3'-dideoxyribonucleosides of four N(6)-substituted purines and 1-deazapurine were prepared using crude nucleoside N-deoxyribosyltransferases (EC 2.4.2.6) from Lactobacillus leichmannii. The 2',3'-dideoxynucleosides derived from N(6)-substituted purines (1-4) are inhibitors of the replication of human immunodeficiency virus type 1 (HIV-1), with EC90 values in the range 20-100 and 20-200 mu m, depending on the cell line used, and have low in vitro toxicity at their effective concentrations.
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收藏
页码:249 / 253
页数:5
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