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Selective inhibition of human immunodeficiency virus (HIV) by 3'-azido-2', 3'-dideoxyguanosine in vitro.

Abstract：

:3'-Azido-2',3'-dideoxyguanosine (AzddGuo) is a potent and selective inhibitor of human immunodeficiency virus (HIV) in vitro. AzddGuo completely inhibits HIV-induced cytopathogenicity and viral antigen expression in MT-4 cells at a concentration of 5.0 microM. Its 50% effective dose for inhibiting HIV-induced cytopathogenicity is 1.4 microM, as compared to 6.4 microM for 2',3'-dideoxyadenosine (ddAdo). Thus, AzddGuo is approximately 4.6-fold more potent as an anti-HIV agent than ddAdo, one of the most promising compounds for the treatment of AIDS. However, AzddGuo is about 4.7 times more cytotoxic than ddAdo, so that its selectivity index, as based on the ratio of the 50% cytotoxic dose to the 50% antiviral effective dose, is almost the same as that of ddAdo (136 and 139, respectively).

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Baba M,Pauwels R,Balzarini J,Herdewijn P,De Clercq E

doi

10.1016/0006-291x(87)91547-6

subject

Has Abstract

pub_date

1987-06-30 00:00:00

pages

1080-6

issue

3

eissn

0006-291X

issn

1090-2104

pii

0006-291X(87)91547-6

journal_volume

145

pub_type

杂志文章

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