EQUAL INHIBITION OF THE REPLICATION OF HUMAN-IMMUNODEFICIENCY-VIRUS IN HUMAN T-CELL CULTURE BY DDA BIS(SATE)PHOSPHOTRIESTER AND 3'-AZIDO-2',3'-DIDEOXYTHYMIDINE

被引:79
作者
PERIGAUD, C
AUBERTIN, AM
BENZARIA, S
PELICANO, H
GIRARDET, JL
MAURY, G
GOSSELIN, G
KIRN, A
IMBACH, JL
机构
[1] FAC MED STRASBOURG,INST VIROL,INSERM,U74,F-67000 STRASBOURG,FRANCE
[2] UNIV MONTPELLIER 2,CHIM BIOORGAN LAB,CNRS,URA 488,F-34095 MONTPELLIER 5,FRANCE
关键词
PRODRUGS; NUCLEOSIDE PHOSPHOTRIESTERS; ANTI-HIV NUCLEOSIDE DERIVATIVES; DIDANOSINE;
D O I
10.1016/0006-2952(94)90217-8
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
It is shown that ddA bis(SATE)phosphotriester is one of the most potent anti-HIV agents in cell culture. Compared with the parent nucleoside, ddA, an increase of 3 orders of magnitude was observed in the EC(50), which makes this compound as active as AZT. This can be tentatively explained if one considers that direct ddAMP intracellular delivery shunts the well established ddA/ddI metabolism pathway.
引用
收藏
页码:11 / 14
页数:4
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