Synthesis of new ent-labdane diterpene derivatives from andrographolide and evaluation on cytotoxic activities

被引:29
作者
Luo, Yan [1 ]
Wang, Ke [2 ,3 ]
Zhang, Meng-han [2 ,3 ]
Zhang, Da-yong [2 ,3 ]
Wu, Yang-chang [4 ]
Wu, Xiao-ming [2 ,3 ]
Hua, Wei-yi [2 ,3 ]
机构
[1] Chinese Acad Sci, High Field Magnet Lab, Hefei 230031, Peoples R China
[2] China Pharmaceut Univ, Ctr Drug Discovery, Nanjing 210009, Jiangsu, Peoples R China
[3] China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Jiangsu, Peoples R China
[4] China Med Univ, Coll Pharm, Grad Inst Pharmaceut Chem, Taichung 40402, Taiwan
基金
中国国家自然科学基金;
关键词
Andrographolide; ent-Labdane diterpene; SAR; Cytotoxic activity; ANALOGS; AGENTS; PANICULATA;
D O I
10.1016/j.bmcl.2015.03.086
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
There are many reports for andrographolide modification regarding antitumor effects. Transformation of the five-membered lactone ring to furan aromatic ring still results in compounds with good cytotoxicity. To determine further the importance of the five-membered lactone ring and to obtain better lead compounds, we transformed the five-membered lactone ring in andrographolide. New types of ent-labdane diterpene derivatives were made, whose cytotoxic activities were measured in vitro. Preliminary SAR was summarized and two compounds, 7 and 26, with good cytotoxic activity were obtained, which have the potential to be developed into new antitumor drugs. (C) 2015 Published by Elsevier Ltd.
引用
收藏
页码:2421 / 2424
页数:4
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