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论文摘要

酚类天然产物Buxifoximes A的合成及生物活性

Total synthesis and biological evaluation of phenolic natural product Buxifoximes A

作者:钟上勇(中北大学化学工程与技术学院 化工综合国家级实验教学示范中心);李星毅(中北大学 化学工程与技术学院 化工综合国家级实验教学示范中心);王艳红(中北大学化学工程与技术学院 化工综合国家级实验教学示范中心);胡志勇(中北大学化学工程与技术学院 化工综合国家级实验教学示范中心);白云丽(中北大学化学工程与技术学院 化工综合国家级实验教学示范中心);荀苗苗(中北大学化学工程与技术学院 化工综合国家级实验教学示范中心);袁长春(中北大学化学工程与技术学院 化工综合国家级实验教学示范中心)

Author:ZHONG Shang-Yong(National Demonstration Center for Experimental Chemical Engineering Comprehensive Education, School of Chemical Engineering and Technology, North University of China);LI Xing-Yi(National Demonstration Center for Experimental Chemical Engineering Comprehensive Education, School of Chemical Engineering and Technology, North University of China);WANG Yan-Hong(National Demonstration Center for Experimental Chemical Engineering Comprehensive Education, School of Chemical Engineering and Technology, North University of China);HU Zhi-Yong(National Demonstration Center for Experimental Chemical Engineering Comprehensive Education, School of Chemical Engineering and Technology, North University of China);BAI Yun-Li(National Demonstration Center for Experimental Chemical Engineering Comprehensive Education, School of Chemical Engineering and Technology, North University of China);XUN Miao-Miao(National Demonstration Center for Experimental Chemical Engineering Comprehensive Education, School of Chemical Engineering and Technology, North University of China);YUAN Chang-Chun(National Demonstration Center for Experimental Chemical Engineering Comprehensive Education, School of Chemical Engineering and Technology, North University of China)

收稿日期:2019-05-13          年卷(期)页码:2020,57(2):348-351

期刊名称:四川大学学报: 自然科学版

Journal Name:Journal of Sichuan University (Natural Science Edition)

关键字:酚类天然产物;酒饼簕;全合成;抗肿瘤活性

Key words:Phenolic natural products;Atalantia buxifolia;Total synthesis;Antitumor activity

基金项目:省自然科学基金

中文摘要

利用商品化试剂4-羟基苯甲酰甲醛水合物(3)为起始原料,与甲氧基胺盐酸盐经一步肟化反应,以79%的收率合成了酚类天然产物Buxifoximes A(1). 同时还经已知反应步骤合成了Buxifoximes A的天然类似物2. 初步的抗肿瘤生物活性测试表明,二者对MV4-11细胞表现出了优秀的抑制作用,同时探讨了构效关系.

英文摘要

Compound 4-hydroxyphenylglyoxal hydrate was chosen as starting material, which can react with N-methoxylamine hydrochloride in one step of oximation reaction, affording phenolic natural product buxifoximes A in yield of 79%. Meanwhile, we also synthesized compound 2, a natural analogue of Buxifoximes A, according to a known procedure. Furthermore, the inhibitory effect of compound and compound 2 on cancer cell proliferation was evaluated and found to possess potent inhibitory activity against MV4-11. Meanwhile, preliminary structure–activity relationships for these two compounds are discussed.

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