Anti-AIDS agents. Part 47: synthesis and anti-HIV activity of 3-substituted 3′,4′-Di-O-(S)-camphanoyl-(3′R,4′R)-(+)-cis-khellactone derivatives

Bioorganic & Medicinal Chemistry Letters
2001.0

Abstract

Six 3-substituted 3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone derivatives (3-8) were synthesized from 3-methyl DCK (2). 3-Hydroxymethyl DCK (6) exhibited potent anti-HIV activity in H9 lymphocytes with EC(50) and TI values of 1.87 x 10(-4) microM and 1.89 x 10(5), respectively. These values are similar to those of DCK and better than those of AZT in the same assay.

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