Nine novel N-piperazinoalkylamide derivatives were synthesized and their structures were con-firmed by ¹H NMR, MS spectra and elemental analysis. All the target compounds, together with the four commercial drugs, naproxen, 4-biphenylacetic acid, brufen (as the acyl agents) and 5-fluorouracil, were tested in vitro for their inhibition on four kinds of human cancer cells, KB, A-549, MDA and Bel-7402. The data showed that all the synthesized compounds exhibited positive effect on KB and Bel-7402 cells, but negative effect on A-549 and MDA cells, while the commercial medicines had the similar results unexpectedly. In addition, the inhibition rate of 4-biphenylacetic acid and naproxen on Bel-7402 cell was equivalent with 5-fluorouracil, while their inhibition on KB cell was higher than that of 5-fluorouracil. The inhibitory ability of the samples on tyrosine kinase was also measured, however no obvious effect was found. The fluorescence spectra of 13a and 4-biphenylacetic acid demonstrated that 13a did not show the interaction with DNA while 4-biphenylacetic acid exhibited the intercalary effect on DNA.

Key words: biological activity, synthesis, polyamine