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 李星毅 王艳红 胡志勇 白云丽 荀苗苗 袁长春 ZHONG Shang-Yong;LI Xing-Yi;WANG Yan-Hong;HU Zhi-Yong;BAI Yun-Li;XUN Miao-Miao;YUAN Chang-Chun(National Demonstration Center for Experimental Chemical Engineering Comprehensive Education, School of Chemical Engineering and Technology, North University of China, Taiyuan 030000, China)

机构地区：[1]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

出　　处：《四川大学学报（自然科学版）》2020年第2期348-351,共4页Journal of Sichuan University(Natural Science Edition)

基　　金：山西省自然科学基金(201801D221087);中北大学青年学术带头人支持计划(QX201806)

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.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.

关 键 词：酚类天然产物 酒饼簕 全合成 抗肿瘤活性 

分 类 号：O629.9[理学—有机化学]