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.

背景：合成了三个系列的新型7-氟-4-（1-哌嗪基）喹啉（I1〜I6，II1〜II2和IV1〜IV4）。通过甲基噻唑基咪唑（MTT）分析，在体外针对表达高水平EGFR的三种人类癌细胞系，即SGC-7901细胞，BEL-7402细胞和A549细胞，评估了它们的抗肿瘤活性。

方法：合成，表征和评价三个系列的喹啉衍生物的体外抗肿瘤活性。

结果与讨论：通过光谱分析证实了新合成化合物的结构。初步的生物测定表明，化合物I1，I10和II1的抗肿瘤活性优于其余目标化合物和吉非替尼针对基于A549细胞的测定，表明化合物I，I10和II1是潜在的癌症治疗药物。结果表明，哌嗪基上的替代物显着影响抗肿瘤活性。

结论：这些结果对于发现更有效的新型抗肿瘤化合物是有用的，并且正在进行进一步的研究。