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Chin. J. Org. Chem. ›› 2012, Vol. 32 ›› Issue (08): 1468-1472.DOI: 10.6023/cjoc201203003 Previous Articles     Next Articles

Articles

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

胡扬根a,b, 高海涛b, 王刚a, 王燕c, 屈永年b, 徐靖b   

  1. a 湖北医药学院附属太和医院药学部 十堰 442000;
    b 湖北医药学院医学化学研究所 十堰 442000;
    c 湖北医药学院基础医学研究所 十堰 442000
  • 收稿日期:2012-03-20 修回日期:2012-04-11 发布日期:2012-04-17
  • 通讯作者: 胡扬根, 徐靖 E-mail:huyangg111@yahoo.com.cn;jxu6686@yahoo.com.cn
  • 基金资助:

    湖北省科技厅自然科学基金(No. 2011CDB08301)、湖北省教育厅研究(Nos. D20092406, Q20102110)和湖北医药学院优秀中青年科技创新团队研究(Nos. 2011CXX03, 2009QDJ15)资助项目.

Synthesis and Antitumor Activity of Some 2-Amino-furo[2,3-d]- yrimidin-4(3H)-one Derivatives

Hu Yanggena,b, Gao Haitaob, Wang Ganga, Wang Yanc, Qu Yongnianb, Xu Jingb   

  1. a Department of Pharmacy, Taihe Hospital of Hubei University of Medicine, Shiyan 442000;
    b Institute of Medicinal Chemistry, Hubei University of Medicine, Shiyan 442000;
    c Institute of Basic Medical Sciences, Hubei University of Medicine, Shiyan 442000
  • Received:2012-03-20 Revised:2012-04-11 Published:2012-04-17
  • Supported by:

    Project supported by the Natural Science Foundation of Hubei Provincial Department of Science and Technology (No. 2011CDB08301), the Science Research Project of Hubei Provincial Department of Education (Nos. D20092406, Q20102110) and the Science and Technology Innovation Team Project of Hubei University of Medicine (Nos. 2011CXX03, 2009QDJ15).

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In this paper, a novel series of 2-aminofuro[2,3-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 IC50 18.4 mmol/L.

Key words: furo[2,3-d]pyrimidin-4(3H)-one, synthesis, antitumor activity