Background: Three series of new 7-fluoro-4-(1-piperazinyl) quinolines (I1~I6, II1~II2 and
IV1~IV4) were synthesized. Their anti-tumor activity was evaluated in vitro against three human
carcinoma cell lines, namely SGC-7901 cells, BEL-7402 cells and A549 cells expressing high levels of
EGFR by Methyl Thiazolyl Terazolium (MTT) assay.
Methods: Three series of quinoline derivatives were synthesized, characterized and evaluated for their
in vitro anti-tumor activities.
Results and Discussion: Structures of the newly synthesized compounds were confirmed by spectral
analysis. The preliminary bioassay indicated that compounds I1, I10 and II1 exhibited better anti-tumor
activity than the rest of the target compounds and gefitinib against A549 cell based assay, which
demonstrated that compounds I1, I10 and II1 are potential agents for cancer therapy. Results suggested
that the substitutes on piperazinyl influenced anti-tumor activities remarkably.
Conclusion: These results are useful for discovering more potent novel anti-tumor compounds and
further studies are ongoing.