有机化学 ›› 2017, Vol. 37 ›› Issue (8): 1952-1963.DOI: 10.6023/cjoc201704004 上一篇    下一篇

综述与进展

核外氮杂甾体的合成及其抗肿瘤活性研究进展

余斌a,b,c, 蔡祖恽d, 王帅a,b,c, 刘宏民a,b,c   

  1. a 郑州大学药学院 郑州 450001;
    b 药物关键制备技术教育部重点实验室 郑州 450001;
    c 新药创制与药物安全性评价河南省协同创新中心 郑州 450001;
    d 上海闵行航北路180弄55号601室 上海 201105
  • 收稿日期:2017-04-05 修回日期:2017-04-21 发布日期:2017-05-02
  • 通讯作者: 刘宏民 E-mail:liuhm@zzu.edu.cn
  • 基金资助:

    国家自然科学基金(Nos.81430085,21372206)、国家重点研发计划(No.2016YFA0501800)、河南省重大科技专项(No.1611003110100)、教育部博士点基金(No.20134101130001)资助项目及郑州大学青年教师启动基金(No.32210533)资助项目.

Recent Advances on the Synthesis and Antitumor Evaluation of Exonuclear Heterosteroids

Yu Bina,b,c, Cai Zuyund, Wang Shuaia,b,c, Liu Hongmina,b,c   

  1. a School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001;
    b Key Laboratory of Advanced Drug Preparation Technologies(Zhengzhou University), Ministry of Education, Zhengzhou 450001;
    c Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Zhengzhou 450001;
    d Room 601 No. 55, Hangbei Road 180, Minhang District, Shanghai 201105
  • Received:2017-04-05 Revised:2017-04-21 Published:2017-05-02
  • Contact: 10.6023/cjoc201704004 E-mail:liuhm@zzu.edu.cn
  • Supported by:

    Received April 5, 2017; revised April 21, 2017; published online May 2, 2017. Project supported by the National Natural Science Foundation of China (Nos. 81430085, 21372206), the National Key Research Program of Proteins (No. 2016YFA0501800), the Key Research Program of Henan Province (No. 1611003110100), the PhD Educational Award from Ministry of Education (No. 20134101130001), and the Starting Grant of Zhengzhou University (No. 32210533).

合成氮杂甾体并评估其生物学活性是甾体化学和甾体新药研发领域的热点之一.通过总结近期发表的相关文献,重点介绍核外氮杂甾体如甾体螺吲哚酮类化合物、三氮唑连接的甾体杂合体及天然氮杂甾体的合成及其抗肿瘤活性的最新进展.

关键词: 氮杂甾体, 合成方法, 抗肿瘤活性

The synthesis and biological evaluation of exonuclear heterosteroids are highly pursued in steroid chemistry and steroid-based new drug design. In this review, the recent progress on the synthesis and antitumor activity of exonuclear heterosteroids is highlighted with particular emphasis on steroidal the spirooxindoles, triazole-linked steroidal conjugates and natural N-heterosteroids.

Key words: steroidal heterocycles, synthetic methods, antitumor activity