Design,synthesis and antitumor activity of 3-substituted quinolone derivatives (Ⅰ)

被引:1
作者
Hua Wang Qi Dong You Zhi Yu Li Yi Quan Zou Department of Medicinal Chemistry
机构
基金
中国国家自然科学基金;
关键词
Quinolone derivatives; Synthesis; Antitumor;
D O I
暂无
中图分类号
O625.31 [酚及其衍生物];
学科分类号
070303 ; 081704 ;
摘要
A series of quinolone derivatives containing benzimidazole,benzoxazole or benzothiazole ring were synthesized.The cytotoxicity of 12 new compounds was evaluated in KB,Be17402,A2780 and HT-29 cell lines.Most of synthesized compounds showed moderate inhibitory activity against cancer cells.The inhibitory activities of 6k,against KB and A2780 tumor cells are comparable to that of topotecan,one of topoisomeraseⅠinhibitors.
引用
收藏
页码:1395 / 1397
页数:3
相关论文
共 12 条
  • [1] H.Koga,A.Itob,S.Murayama,et al. J.Meal.Chem . 1980
  • [2] H.J.Park,Y.S.Kim,J.S.Kim,et al. Bioorg.IVied.Chem.Lett . 2004
  • [3] B.K.Sinha. Drugs . 1995
  • [4] The Use of Polyphosphoric Acid in the Sythesis of 2-Aryl-substituted Benzimid-azoles,Benzoxzoles and Benzothiazoles. Hein,D.W,R.J Alheim,J.J.Leavitt. Journal of the American Chemical Society . 1957
  • [5] Effects of novel fluoroquinolones on the catalytic activities of eukaryotic Topisomerasell.Influence of the C-8 fluorine group. Robinson MJ,Martin BA,Gootz TD,et al. Antimicrobial Agents and Chemotherapy . 1992
  • [6] Structure–activity relationships of benzimidazoles and related heterocycles as topoisomerase I poisons. Kim,JS,Sun,Q,Gatto,B,Yu,C,Liu,A,Liu,LF,LaVoie,EJ. Bioorganic and Medicinal Chemistry . 1996
  • [7] DNA topoisomerase poisons as antitumor drugs. Liu,LF. Annual Review of Biochemistry . 1989
  • [8] I.Mozk,B.Sket. J.Heterocycl.Chem . 1994
  • [9] L.A.Mitscher,H.E.Gracey,G.W.Clark,et al. J.Meal.Chem . 1978
  • [10] M.R.Redinbo,J.J.Champoux,G.J.Wire. Biochemistry . 2000