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新型喹诺酮类化合物的设计合成与生物活性研究

Design,synthesis and biological evaluation of novel quinolones

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【作者】 高佳娣方成汤雁波肖志艳

【Author】 GAO Jia-di,FANG Cheng,TANG Yan-bo,XIAO Zhi-yan(Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation & Institute of Materia Medica,Peking Union Medical College and Chinese Academy of Medical Sciences,Beijing 100050,China)

【机构】 北京协和医学院中国医学科学院药物研究所活性物质发现与适药化研究北京市重点实验室

【摘要】 目的设计合成具有抗肿瘤和抗HIV活性的新型喹诺酮类化合物。方法邻苯二胺衍生物和苯甲酰乙酸乙酯衍生物经缩合关环反应得到目标产物。结果与结论共合成5个未见文献报道的喹诺酮类化合物(7~11),目标化合物的结构经1H-NMR、ESI-MS谱确证。并利用谱学方法解析了此类化合物的互变异构现象。其中,化合物11具有明显的抗肿瘤及抗HIV活性。

【Abstract】 As a privileged structure,the quinolone scaffold is well-presented in a variety of therapeutic drugs and bioactive agents.The design and synthesis of novel quinolones as simplified analogues of the anticancer agent flavopiridol were described herein.Five novel quinolone derivatives were prepared via cyclizative condensation between the aniline derivative 3 and the β-oxa-ester 6.The structures of the target compounds(7-11) were confirmed by 1H-NMR and ESI-MS data,and tautomerism of the quinolone scaffold was observed and elucidated with spectral methods.Compound 11 showed an apparent antitumor activity in the SRB assay(GI50=17.28-33.72 μmol · L-1) and it also exhibited noticeable anti-HIV activities with EC50 and CC50 values of 21.04 μmol · L-1 and 21.49 μmol · L-1,respectively.

【基金】 国家自然科学基金项目(81172985)
  • 【文献出处】 中国药物化学杂志 ,Chinese Journal of Medicinal Chemistry , 编辑部邮箱 ,2013年01期
  • 【分类号】R914.5;R96
  • 【下载频次】136
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