色酮吡唑啉酮类衍生物的合成及抗白血病细胞活性  

Synthesis and Anti-human Leukemia Cells Proliferative Activities of Pyrazolone-Chromone Derivatives

作　　者：王楠馨 汪军鑫 田民义 刘雄利[1] 邓国栋[1] WANG Nan-xin;WANG Jun-xin;TIAN Min-yi;LIU Xiong-li;DENG Guo-dong(National&Local Joint Engineering Research Center for the Exploition of Homology Resources of Medicine and Food,Guizhou University,Guiyang 550025,China)

机构地区：[1]贵州大学西南药食两用资源开发利用技术国家地方联合工程研究中心,贵州贵阳550025

出　　处：《合成化学》2021年第3期214-220,共7页Chinese Journal of Synthetic Chemistry

基　　金：贵州大学培育项目(黔科合平台人才[2018]5781号)。

摘　　要：以色酮-吡唑啉酮作为C1合成子,在5 mol%的DBU催化下,与α,β-不饱和酮发生Michael加成反应,获得了10个色酮吡唑啉酮类衍生物3a~3j,产率76%~90%,dr值为4/1~9/1,其结构经^(1)H NMR,^(13)C NMR和HR-MS(ESI-TOF)表征,通过单晶进一步进行了确定化合物3b的相对构型。该类化合物包含有连续两个立体中心,包括一个季碳中心,可以为生物活性筛选提供物质基础。采用MTT法研究了3a~3f对人白血病细胞(K562)的体外抗增殖活性。结果表明:化合物3a,3c,3d和3i对K562增殖具有一定的抑制活性。In this paper,the Michael addition reaction of pyrazolone-chromone C1 synthons withα,β-unsaturated ketones was investigated,using DBU as an organic catalyst,to provide a variety of pyrazolone-chromone derivatives(3a~3j)in 76%~90%yields and 4/1~9/1 dr.The structures of products 3 were characterized by^(1)H NMR,^(13)C NMR and HR-MS(ESI-TOF).The relative configuration of compound 3b was further determined by the single crystal.The in vitro anti-proliferative activities against human leukemia cells(K562)were demonstrated by MTT assays using the commercially available broad-spectrum anticancer drug Cisplatin as a positive control.The results showed that compounds 3a,3c,3d and 3i showed good cytotoxic effects.

关 键 词：色酮-吡唑啉酮 Α Β-不饱和酮 二氮杂二环 色酮吡唑啉酮类衍生物 抗白血病细胞活性 合成 

分 类 号：O626.13[理学—有机化学] O623.7[理学—化学]