Abstract:
In an effort to establish new candidates with enhanced anticancer activity of 5-hydroxy-7-methyl-1,4-
naphthoquinone scaffold (7-methyljuglone) previously isolated from the root extract of Euclea natalensis,
a series of 7-methyljuglone derivatives have been synthesized and assessed for cytotoxicity on selected
human cancer lines. These compounds were screened in vitro for anticancer activity on MCF-7, HeLa, SNO
and DU145 human cancer cell lines by MTT assay. Most of them exhibited significant toxicity on cancer
cell lines with lower IC50 values. The most potent derivative (19) exhibited the toxicity on HeLa and
DU145 cell lines with IC50 value of 5.3 and 6.8 lM followed by compound (5) with IC50 value of 10.1
and 9.3 lM, respectively. Structure–activity relationship reveals that the fluoro substituents at position
C-8 while hydroxyl substituents at C-2 and C-5 positions played an important role in toxicity.
