| Abstract
| - Twenty-eight compounds related to dehydrozingerone (1), isoeugenol (3), and 2-hydroxychalcone (4) were synthesizedand 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 IC50 value of0.6 μg/mL. Furthermore, dehydrozingerone analogue 11 and chalcones 16 and 17 showed significant and similar cytotoxicactivity against both KB (IC50 values of 2.0, 1.0, and 2.0 μg/mL, respectively) and KB-VCR (IC50 values of 1.9, 1.0,and 2.0 μg/mL, respectively) cells, suggesting that they are not substrates for the P-glycoprotein drug efflux pump.
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