Synthesis and anti-HIV activity of 4'-thio-2',3'-dideoxynucleosides
- 1 February 1992
- journal article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 35 (3) , 533-538
- https://doi.org/10.1021/jm00081a015
Abstract
A series of 2',3'-dideoxy-4'-thionucleoside analogues of purines and pyrimidines, including 4'-thioddI (17), 4'-thioddC (27), and 4'-thioAZT (34), were synthesized and evaluated for their inhibitory activity against human immunodeficiency virus (HIV). A stereospecific synthesis of the 2,3-dideoxy-4-thioribofuranosyl carbohydrate precursor 11 starting with L-glutamic acid is described. 2',3'-Dideoxy-4'-thiocytidine (27) displayed significant, but modest activity in vitro against human immunodeficiency virus.Keywords
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