Prodrug design, synthesis and pharmacokinetic evaluation of (3' R, 4' R)-3-hydroxymethyl-4-methyl-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone.


3-Hydroxymethyl-4-methyl-DCK (3, HMDCK) was discovered previously as a potent HIV non-nucleoside reverse transcriptase inhibitor (NNRTIs) (EC50: 0.004 μM, TI: 6225) with a novel mechanism of action. It exerts anti-HIV activity by inhibiting the production of HIV-1 double-stranded viral DNA from a single-stranded DNA intermediate, rather than blocking the… (More)