Synthesis and Antitumor Activity of Diosgenin Hydroxamic Acid and Quaternary Phosphonium Salt Derivatives

被引:7
作者
Wang, Lin [1 ]
Yao, Maoling [1 ]
Hu, Yuegao [1 ]
Chen, Congdi [2 ]
Jin, Liming [1 ]
Ma, Xiaodong [2 ]
Yang, Hongjun [1 ]
机构
[1] Southwest Minzu Univ, Sch Chem & Environm, Natl Ethn Affairs Commiss, Key Lab Gen Chem, Chengdu 610041, Peoples R China
[2] Dalian Med Univ, Coll Pharm, Dalian 116044, Peoples R China
关键词
Diosgenin; antitumor; derivatives; quaternary phosphonium salt; hydroxamic acid; BIOLOGICAL EVALUATION; SARSASAPOGENIN DERIVATIVES; STEROIDAL DERIVATIVES; DESIGN; AGENTS;
D O I
10.1021/acsmedchemlett.1c00581
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Diosgenin, a component separated from Dioscorea plants, is an important starting material for steroid hormone drugs and semisynthetic steroids. In the work, two series of diosgenin derivatives were designed, synthesized, and evaluated for their cellular anticancer activities. Most of the target compounds exhibited good inhibitory activities against four cell lines, Aspc-1 (human and SW620 (human metastatic pancreatic cancer cells). Among them, the representative compound 2.2f exhibited 7.9-341.7-fold antiproliferative activities against the above-mentioned four cell lines compared with the lead compound diosgenin.
引用
收藏
页码:786 / 791
页数:6
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