Synthesis and anti-HIV activity of various 2'-and 3'-substituted 2', 3'-dideoxyadenosines: a structure-activity analysis

P Herdewijn, R Pauwels, M Baba…

文献索引：Herdewijn; Pauwels; Baba; Balzarini; De Clercq Journal of Medicinal Chemistry, 1987 , vol. 30, # 11 p. 2131 - 2137

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被引用次数: 158

摘要

A systematic synthesis was undertaken of 2', 3'-dideoxyadenosine analogues with either an azido, fluorine, or hydroxyl group substituted in the “up” or “downn position of C-2 or C-3 of the sugar moiety. The compounds were evaluated against the cytopathogenicity of human immunodeficiency virus (HIV) for MT-4 cells. The four azido derivatives 6, 7, 8, and 9 were synthesized by a nucleophilic displacement reaction with lithium azide on the mesylates 3, ...