有机化学 ›› 2013, Vol. 33 ›› Issue (01): 169-173.DOI: 10.6023/cjoc201208037 上一篇    下一篇

研究简报

山荷叶素异羟肟酸和硫醇衍生物的合成与抑制肿瘤细胞增殖活性

赵育, 倪春燕, 张虞婷, 朱俐   

  1. 南通大学航海医学研究所 南通 226001
  • 收稿日期:2012-08-31 修回日期:2012-09-24 发布日期:2012-10-09
  • 通讯作者: 朱俐 E-mail:zhulili65@163.com
  • 基金资助:

    江苏省自然科学基金(No. BK2011390);江苏省高校优势学科(PAPD)资助项目.

Synthesis and Antiproliferatory Activity of Novel Diphyllin Hydroxamic Acid and Mercaptan Derivatives

Zhao Yu, Ni Chunyan, Zhang Yuting, Zhu Li   

  1. Institute of Nautical Medicine, Nantong University, Nantong 226001
  • Received:2012-08-31 Revised:2012-09-24 Published:2012-10-09
  • Supported by:

    Project supported by the Natural Science Foundation of Jiangsu Province (No. BK2011390) and the Priority Academic Program Development of Jiangsu Higher Education Instititutions (PAPD).

通过药效团整合策略将天然抗肿瘤活性木脂素山荷叶素与组蛋白去乙酰化酶抑制剂的药效团长链异羟肟酸或长链硫醇进行拼合, 得到了7个未见文献报道的山荷叶素衍生物, 通过核磁共振氢谱、碳谱、高分辨质谱等方法进行了结构表征. 并采用了噻唑蓝法(MTT)法对这些化合物的体外抑制肿瘤细胞增殖活性进行了测试, 异羟肟酸类衍生物具有较强的活性.

关键词: 山荷叶素, 组蛋白去乙酰化酶抑制剂, 抗肿瘤, 合成

Seven novel diphyllin derivatives have been synthesized by incorporating histone deacetylase inhibitory functional groups into diphyllin. The structures were confirmed by 1H NMR, 13C NMR and HRMS. Their antiproliferative activity against three human cancer cell lines was investigated by methyl thiazolyl tetrazoliym (MTT) assay.

Key words: diphyllin, histone deacetylase inhibitors, antitumor, synthesis