Anti-aids agents 33. 1 Synthesis and anti-HIV activity of mono-methyl substituted 3′, 4′-di-O-(−)-camphanoyl-(+)-cis-khellactone (DCK) analogues

L Xie, Y Takeuchi, LM Cosentino, KH Lee

文献索引：Xie, Lan; Takeuchi, Yasuo; Cosentino, L. Mark; Lee, Kuo-Hsiung Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 16 p. 2151 - 2156

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被引用次数: 30

摘要

Four isomeric methyl substituted DCK analogues (2–5) were asymmetrically synthesized from different starting materials. 3-Methyl, 4-methyl, and 5-methyl-3′, 4′-di-O-(−)- camphanoyl-(+)-cis-khellactone (2–4) all were extremely potent against HIV-1 replication in H9 lymphocyte cells with EC50 and therapeutic index values of< 4.23× 10− 7 μM and> 3.72× 108, respectively, which are much better than those of DCK and AZT in this assay.