Abstract��OBJECTIVE To study the synthesis and antitumor activity of novel quinolone derivatives. METHODS Based on the structure of ciprofloxacin, the objective substances were designed and synthesized according to the principle of fragment-based drug discovery. Their anti-tumor activities in vitro were evaluated against A549, HL-60, and Hela cells by MTT assay. Molecular docking studies were performed with the Libdock protocol of Discovery Studio to afford the ideal interaction mode of the compound with the binding site of the Topo ��. RESULTS Eight novel compounds were synthesized and showed potential antitumor activities. CONCLUSION The antitumor activities of the synthesized quinolone derivatives are worthy of further study.
ERTL P, JELFS S, M��HLBACHER J, et al. Quest for the rings. In silico exploration of ring universe to identify novel bioactive heteroaromatic scaffolds [J]. J Med Chem, 2006, 49(15):4568-4573.
[2]
SISSI C,PALUMBO M. The quinolone family:from antibacterial to anticancer agents [J]. Curr Med Chem Anticancer Agents, 2003, 3(6):439-450.
[3]
MUGNAINI C, PASQUINI S, CORELLI F. The 4-quinolone-3-carboxylic acid motif as a multivalent scaffold in medicinal chemistry [J]. Curr Med Chem, 2009, 16(14):1746-1767.
[4]
XU Q J, HOU L L, WU Z F, et al. Synthesis and antitumor evaluation of fluoroquinolon C3 s-triazole oxadizaole methylsufide derivatives of ofloxacin [J]. Chin Pharm J(�й�ҩѧ��־), 2014, 49(7):609-612.
[5]
LI T, GAO L Z, XIE Y S, et al. Synthesis and antitumor activity fluoroquinolon-3-yloxadiazole sulfanylacetylhydrazone derivatives [J]. Chin Pharm J(�й�ҩѧ��־), 2014, 49(24):2206-2209.
[6]
GAO L Z, LI T, XIE Y S, et al. Synthesis and antitumor activity of fluoroquinolone-3-yl s-triazole sulfanylacetylhydrazones and s-triazole hydrazone derivatives (V) [J]. Chin Pharm J(�й�ҩѧ��־), 2015, 50(6):545-549.
[7]
YOU Q D, LI Z Y, HUANG C H, et al. Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification [J]. J Med Chem, 2009, 52(18):5649-5661.
[8]
LI J, JIN Y, SHOU K J, et al. Design, synthesis and antitumor activity of quinolone derivatives [J]. Chin Pharm J(�й�ҩѧ��־), 2013, 48(23):2055-2060.
[9]
GUO H Y, TIAN Z M, SUN L Y, et al. Synthesis of difloxacin hydrochloride [J]. Chin J Pharm(�й�ҽҩ��ҵ��־),1992, 23(12):529-531.
[10]
GIOVANELLA B C, STEHLIN J S, WALL M E, et al. DNA topoisomerase I-Targeted chemotherapy of human colon cancer in xenografts [J]. Science, 1989, 246(4933):1046-1048.
2016, Vol. 51 
