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期刊论文
ANTI-AIDS AGENTS 31.1 SYNTHESIS AND ANTI-HIV ACTIVITY OF 4-SUBSTITUTED 3', 4'-DI-O-(-)-CAMPHANOYL-(+)-Cis-KHELLACTONE (DCK) THIOLACTONE ANALOGS
Bioorganic & Medicinal Chemistry Letters 8(1998)1483-1486,-0001,():
Four DCK-thiolactone analogs (3-6) Were synthesized asymmetrically and evaluated for anti-HIV activity against HIV-1 replication in H9 lymphocyte cells. Based on the functionality on the thiolactone-coumarin nucleus, activity was in the order: methyl>H>propyl>benzyl. 4-Methyl-3',4'-di-O-(-)-camphanoyl-(+)-cis-khelthiolactone (4) exhibited extremely potent anti-HIV activity with EC50 and therapeutic index values of 0.00718μM and>21,300, respectively.
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