Abstract
Some 1,4-napthoquinone derivatives were synthesized, and dimers of 5-hydroxy-7-methyl-1,4-naphthoquinone (5) were isolated from the roots of Euclea natalensis. Their structures were confirmed by spectroscopic (UV, IR, NMR, and MS) analysis. The HIV-1 reverse transcriptase inhibition activity of the compounds against recombinant HIV-1 enzyme was studied in vitro (non-radioactive HIV-RT colorimetric assay) using the Roche Diagnostic kit and compared with that of doxorubicin as standard drug. Some of the synthesized compounds exhibited exceptionally potent (91–100%) HIV-1 RT inhibition at 100 μg/mL concentration. Surprisingly the dimers showed very weak activity.
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