Chin. J. Org. Chem. ›› 2014, Vol. 34 ›› Issue (11): 2362-2369.DOI: 10.6023/cjoc201405018 Previous Articles     Next Articles



陈玉a, 柏舜a, 贺红武b, 杨光忠c   

  1. a 中南民族大学化学与材料科学学院 武汉 430074;
    b 华中师范大学化学学院 武汉 430079;
    c 中南民族大学药学院 武汉 430074
  • 收稿日期:2014-05-12 修回日期:2014-06-17 发布日期:2014-07-03
  • 通讯作者: 杨光忠,
  • 基金资助:


Synthesis and Antitumor Activity Evaluation of Novel Tetrahydro-[4,5]benzothieno[2,3-d]pyrimidinone Derivatives

Chen Yua, Bai Shuna, He Hongwub, Yang Guangzhongc   

  1. a College of Chemistry and Materials Science, South-Central University for Nationalities, Wuhan 430074;
    b College of Chemistry, Central China Normal University, Wuhan 430079;
    c College of Pharmacy, South-Central University for Nationalities, Wuhan 430074
  • Received:2014-05-12 Revised:2014-06-17 Published:2014-07-03
  • Supported by:

    Project supported by the Special Fund for Basic Scientific Research of Central Colleges, South-Central University for Nationalities (No.CZY13004).

Six 3-alkyl-5,6,7,8-tetrahydro[4,5]benzothieno[2,3-d]pyrimidin-4-one derivatives and seventeen 3-benzylidene- aminotetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-one derivatives have been designed and synthesized via Gewald reaction under mild condition. The structures of synthesized compounds were characterized by 1H NMR, 13C NMR, IR and MS. Their antitumor activities were evaluated against human nasopharyngeal carcinoma (KB) and human nasopharyngeal carcinoma (CNE2) cell lines in vitro. These results revealed that four tested compounds showed moderate antitumor activities.

Key words: thieno[2,3-d]pyrimidinone derivatives, antitumor activity, Gewald reaction