Citation: Luo Zhuoma, Hu Yuegao, Wang Luhong, Yin Xiangjian, Ma Xiaodong, Yang Hongjun, Zhao Zhigang. Study on the Synthesis and Bioactivity of Diosgenin Antitumor Derivatives[J]. Chinese Journal of Organic Chemistry, ;2018, 38(4): 919-925. doi: 10.6023/cjoc201711016 shu

Study on the Synthesis and Bioactivity of Diosgenin Antitumor Derivatives

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

Corresponding author: Yang Hongjun, yanghj@swun.cn
Received Date: 8 November 2017
Revised Date: 5 January 2018
Available Online: 18 April 2018
Fund Project: the Southwest University for Nationalities Graduate Student Innovative Project CX2016SZ045the National Natural Science Foundation of China 21602083Project 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)the Sichuan Provincial Department of Education Research Project 15ZB0487

Figures(3)

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.
- diosgenin,
- derivative,
- antitumor activity,
- amide
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