Twenty-eight compounds related to dehydrozingerone (
1), isoeugenol (
3),
and 2-hydroxychalcone (
4) were synthesized
and evaluated in vitro against human tumor cell replication. Except for isoeugenol analogues
27-
35, most compoundsexhibited moderate or strong cytotoxic activity against KB, KB-VCR (a multidrug-resistant derivative),
and A549 celllines. In particular, chalcone
15 showed significant cytotoxic activity against the A549 cell line with an IC
50 value of0.6
![](/images/entities/mgr.gif)
g/mL. Furthermore, dehydrozingerone analogue
11 and chalcones
16 and 17 showed significant
and similar cytotoxicactivity against both KB (IC
50 values of 2.0, 1.0,
and 2.0
![](/images/entities/mgr.gif)
g/mL, respectively)
and KB-VCR (IC
50 values of 1.9, 1.0,
and 2.0
![](/images/entities/mgr.gif)
g/mL, respectively) cells, suggesting that they are not substrates for the P-glycoprotein drug efflux pump.