Anti-AIDS agents-XXVIII. 1 Synthesis and Anti-HIV activity of methoxy substituted 3′, 4′-Di-O-(−)-camphanoyl-(+)-cis-khellactone (DCK) analogues

Y Takeuchi, L Xie, LM Cosentino, KH Lee

Index: Takeuchi, Yasuo; Xie, Lan; Cosentino, L. Mark; Lee, Kuo-Hsiung Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 20 p. 2573 - 2578

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Citation Number: 44

Abstract

Four isomeric methoxy substituted DCK analogues (3–6) were asymmetrically synthesized from different starting materials. 5-Methoxy-3′, 4′-di-O-(−)-camphanoyl-(+)-cis-khellactone (5) exhibited extremely potent anti-HIV activity against HIV-1 replication in H9 lymphocyte cells with EC50 and therapeutic index values of 0.00038 μM and> 402,632, respectively, which are better than those of DCK and AZT in this assay.