Synthesis and evaluation of novel alkannin and shikonin oxime derivatives as potent antitumor agents

被引:51
作者
Wang, Rubing [1 ]
Zhang, Xu [1 ]
Song, Hualong [1 ]
Zhou, Shanshan [1 ]
Li, Shaoshun [1 ]
机构
[1] Shanghai Jiao Tong Univ, Sch Pharm, Shanghai 200240, Peoples R China
关键词
Alkannin; Shikonin; Oxime derivatives; Antitumor activity; IN-VITRO; BETA-HYDROXYISOVALERYLSHIKONIN; NATURAL-PRODUCTS; APOPTOSIS; INVOLVEMENT; INDUCTION; ANALOGS; CELLS;
D O I
10.1016/j.bmcl.2014.07.012
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A set of forty alkannin and shikonin oxime derivatives were firstly designed and synthesized. Their cytotoxicities against three kinds of tumor cells and a normal cell line were tested and compared with alkannin and shikonin. The cell-based investigation demonstrated that some oxime derivatives were more or comparatively effective to the lead compounds, especially their selective and excellent antitumor activities towards K562 cells with no toxicity in normal cells. We may conclude that oximate modification to the mother nucleus of alkannin and shikonin is an available approach to acquire potent antitumor agents. (C) 2014 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4304 / 4307
页数:4
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