Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (4): 919-925.DOI: 10.6023/cjoc201711016 Previous Articles     Next Articles



罗卓玛a, 胡越高a, 王璐红b, 尹祥健c, 马晓东b, 杨鸿均a, 赵志刚a   

  1. a 西南民族大学化学与环境保护工程学院 成都 610041;
    b 大连医科大学药学院 大连 116044;
    c 四川川大华西药业股份有限公司 成都 610014
  • 收稿日期:2017-11-08 修回日期:2018-01-05 发布日期:2018-01-18
  • 通讯作者: 杨鸿均
  • 基金资助:


Study on the Synthesis and Bioactivity of Diosgenin Antitumor Derivatives

Luo Zhuomaa, Hu Yuegaoa, Wang Luhongb, Yin Xiangjianc, Ma Xiaodongb, Yang Hongjuna, Zhao Zhiganga   

  1. a College of Chemistry and Environmental Protection Engineering, Southwest University for Nationalities, Chengdu 610041;
    b College of Pharmacy, Dalian Medical University, Dalian 116044;
    c Sichuan Chuanda Huaxi Pharmaceutical Co., Ltd., Chengdu 610014
  • Received:2017-11-08 Revised:2018-01-05 Published:2018-01-18
  • Contact: 10.6023/cjoc201711016
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21602083), the Southwest University for Nationalities Graduate Student Innovative Project (No. CX2016SZ045), and the Sichuan Provincial Department of Education Research Project (No. 15ZB0487).

Nine novel diosgenin derivatives were designed and synthesized by using diosgenin as a precursor. Their structures were identified by 1H NMR, 13C NMR, IR and HRMS. Antitumor activity (A549, A431, H1975, HCT-116, Aspc-1, Ramos) and cytotoxicity (HBE, LO-2) were measured for all derivatives using thiazolyl blue tetrazolium bromide (MTT). The results show that most diosgenin derivatives have significant anti-tumor activity and low cytotoxicity.

Key words: diosgenin, derivative, antitumor activity, amide