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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Research Article

Synthesis and Anti-Tumor Activity Evaluation of Novel 7-Fluoro-4-(1- Piperazinyl) Quinolines

Author(s): Dan Liu*, Aiqi Xue, Zhixin Liu, Yi Zhang, Penghui Peng and Haifeng Wang

Volume 16, Issue 6, 2019

Page: [663 - 669] Pages: 7

DOI: 10.2174/1570180815666180820131036

Price: $65


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.

Keywords: 7-fluoro-4-(1-piperazinyl) quinolines, anti-tumor, tyrosine kinase inhibitors, synthesize, cancer therapy, Methyl Thiazolyl Tetrazolium (MTT), carcinoma cell.

Graphical Abstract
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