Chin. J. Org. Chem. ›› 2016, Vol. 36 ›› Issue (7): 1653-1661.DOI: 10.6023/cjoc201601011 Previous Articles     Next Articles

Articles

含亚磺酸酯或亚磺酰胺基团的香豆素衍生物的合成及生物活性研究

刘明a, 刘阳a, 刘艾林b, 张冬凯a, 陈明桂a, 吴长春a, 华学文a, 周莎a, 李正名a   

  1. a. 南开大学元素有机化学研究所 元素有机化学国家重点实验室 天津化学化工协同创新中心 天津 300071;
    b. 北京协和医学院 中国医学科学院药物研究所 北京 100050
  • 收稿日期:2016-01-11 修回日期:2016-02-22 发布日期:2016-03-11
  • 通讯作者: 李正名 E-mail:nkzml@vip.163.com
  • 基金资助:

    高等学校学科创新引智计划(No.B06005)、元素有机化学国家重点实验室和天津化学化工协同创新中心资助项目.

Synthesis and Bioactivities of Novel Coumarin Derivatives Containing Sulfinic Esters or Sulfinamide Moiety

Liu Minga, Liu Yanga, Liu Ailinb, Zhang Dongkaia, Chen Mingguia, Wu Changchuna, Hua Xuewena, Zhou Shaa, Li Zhengminga   

  1. a. State Key Laboratory of Elemento-organic Chemistry, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Institute of Elemento-organic Chemistry, Nankai University, Tianjin 300071;
    b. Institute of Materia Medica, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050
  • Received:2016-01-11 Revised:2016-02-22 Published:2016-03-11
  • Supported by:

    Project supported by the “111” Project of Ministry of Education of China (No. B06005), and the State Key Laboratory of Elemento-organic Chemistry and Collaborative Innovation Center of Chemical Science and Engineering (Tianjin).

A series of novel coumarin derivatives containing sulfinic esters or sulfonamide were designed and synthesized. Their structures were characterized by 1H NMR, 13C NMR and elemental analysis. The preliminary bioassays indicated that several target compounds exhibited good in vitro antitumor activities on A549 (up to 67.82%), Bel7402 (up to 58.47%) and HCT-8 (up to 74.80%) at 5.0 mg/L and moderate antifungal activities on Physalospora piricola (up to 82.0 %) at 50 mg/L. The structure-activity relationship of these target compounds was discussed accordingly.

Key words: coumarin, sulfinic esters, sulfinamide, anticancer activity, antifungal activity