|
|||||
|
|
| 新型2-氨基-呋喃并[2,3-d]嘧啶-4(3H)-酮衍生物的合成及抗肿瘤活性 | |
| 引用本文： | 胡扬根,高海涛,王刚,王燕,屈永年,徐靖.新型2-氨基-呋喃并[2,3-d]嘧啶-4(3H)-酮衍生物的合成及抗肿瘤活性[J].有机化学,2012,31(8):1468-1472. |
| 作者姓名： | 胡扬根 高海涛 王刚 王燕 屈永年 徐靖 |
| 作者单位： | 1. 湖北医药学院附属太和医院药学部 十堰442000;湖北医药学院医学化学研究所 十堰442000 2. 湖北医药学院医学化学研究所 十堰442000 3. 湖北医药学院附属太和医院药学部 十堰442000 4. 湖北医药学院基础医学研究所 十堰442000 |
| 基金项目： | 湖北省科技厅自然科学基金，湖北省教育厅研究，湖北医药学院优秀中青年科技创新团队研究 |
| 摘 要： | 报道应用aza-Wittig反应,采用易得的原料,在温和的条件下,以78%～90%的产率有效的合成了新型2-氨基-呋喃并3,2-d]嘧啶-4(3H)-酮衍生物5,其结构经IR,1H NMR,MS和元素分析确认.为进一步得到结构确认,化合物5c经X射线衍射分析证实.运用噻唑蓝(MTT)标准法对化合物5进行了体外抗肿瘤活性的测定,其中5f对肺癌细胞A459的IC50值为18.4μmol/L,显示出潜在良好的抗肿瘤活性. |
| 关 键 词： | 呋喃并[2 3-d]嘧啶-4(3H)-酮 合成 抗肿瘤活性 |
Synthesis and Antitumor Activity of Some 2-Amino-furo[2,3-d]-yrimidin-4(3H)-one Derivatives |
|
| Hu Yanggen , Gao Haitao , Wang Gang , Wang Yan , Qu Yongnian , Xu Jing.Synthesis and Antitumor Activity of Some 2-Amino-furo[2,3-d]-yrimidin-4(3H)-one Derivatives[J].Chinese Journal of Organic Chemistry,2012,31(8):1468-1472. | |
| Authors: | Hu Yanggen Gao Haitao Wang Gang Wang Yan Qu Yongnian Xu Jing |
| Institution: | ,b(aDepartment of Pharmacy,Taihe Hospital of Hubei University of Medicine,Shiyan 442000)(bInstitute of Medicinal Chemistry,Hubei University of Medicine,Shiyan 442000)(cInstitute of Basic Medical Sciences,Hubei University of Medicine,Shiyan 442000) |
| Abstract: | In this paper,a novel series of 2-aminofuro2,3-d]yrimidin-4(3H)-one derivatives were prepared via aza-Wittig reaction of iminophosphorane 3 with aromatic isocyanate and subsequent reaction with various amine under mild condition in 78%～90% yields.The structures of these compounds were confirmed by mass spectral data,1H NMR,IR and elemental analysis.Compound 5c was further analyzed by single crystal X-ray diffraction.The in vitro antitumor activities of compounds 5 were analyzed with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide(MTT) standard method,and compound 5f showed the best inhibition activities against A459 with IC5018.4 μmol/L. |
| Keywords: | furo[2 3-d]pyrimidin-4(3H)-one synthesis antitumor activity |
| 本文献已被 CNKI 万方数据 等数据库收录！ | |