Synthesis and Antitumor Evaluation of 3-epi-Jaspine B Analogues

被引:2
|
作者
Zhang En [1 ]
Wang Shang [1 ]
Jiao Weiwei [1 ]
Wang Mingming [1 ]
Yue Jingfei [1 ]
Xu Shuaimin [1 ]
Wang Ya'na [1 ]
Ambrosi, Horst-Dieter [2 ]
Liu Hongmin [1 ]
机构
[1] Zhengzhou Univ, Sch Pharmaceut Sci, Collaborat Innovat Ctr New Drug Res & Wily Evalua, Zhengzhou 450001, Peoples R China
[2] AnalytiCon Discovery GmbH, Hermannswerder Haus 17, D-14473 Potsdam, Germany
基金
中国国家自然科学基金;
关键词
3-epi-jaspine B; antitumor; hydrogen sulfide; analogue; PACHASTRISSAMINE JASPINE B; BIOLOGICAL EVALUATION; MARINE SPONGE; DERIVATIVES; INHIBITORS; EFFICIENT; DESIGN;
D O I
10.6023/cjoc201607028
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Jaspine B is a natural product with significant antitumor activity, which was isolated from the marine sponge Pachastrissa sp. In order to find new antitumor compounds with high efficiency and succinct synthetic methods, a series of 3-epi-jaspine B analogues were designed and synthesized. 16 compounds were synthesized and all of them were unknown in the literature. Their structures were determined by H-1 NMR, C-13 NMR and HRMS. The antitumor activity of these compounds against four tumor cell lines B16 -F10, A-549, MCF-7 and PC -3 was assayed using thiazolyl blue (MTT) assay, and some compounds showed potent inhibitory effect on tumor cells. Compounds 8f and 11 were more potent against A-549 with IC50 of (9.646 +/- 0.984) and (7.144 +/- 0.854) mu g/mL.
引用
收藏
页码:141 / 148
页数:8
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