新型四氢苯并[4,5]噻吩并[2,3-d]嘧啶酮衍生物的合成及其抗肿瘤活性有机化学.pdfVIP

DOI: 10.6023/cjoc201405018 研究简报 有机化学 Chinese Journal of Organic Chemistry NOTE 新型四氢苯并[4,5]噻吩并[2,3-d]嘧啶酮衍生物的合成及其抗肿瘤活性 陈 玉a 柏 舜a 贺红武b 杨光忠*,c (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) 摘要 以环己酮为原料, 利用 Gewald 反应合成了 6 个 3-烷基-5,6,7,8- 四氢苯并[4,5]噻吩并[2,3-d]嘧啶-4-酮衍生物和 17 个 3-亚苄基胺基四氢苯并[4,5]噻吩并[2,3-d]嘧啶-4-酮衍生物, 通过 1 13 H NMR 、 C NMR、IR 和 MS 对所合成的化合物 进行了结构表征, 并对所合成化合物进行了抗肿瘤活性的筛选. 结果表明 4 个化合物对人鼻咽癌细胞株(KB)和鼻咽鳞 癌细胞株(CNE2)两种肿瘤细胞株表现出一定程度的抑制活性. 关键词 噻吩并[2,3-d]嘧啶酮衍生物; 抗肿瘤活性; Gewald 反应 Synthesis and Antitumor Activity Evaluation of Novel Tetrahydro- [4,5]benzothieno[2,3-d]pyrimidinone Derivatives Chen, Yua Bai, Shun a He, Hongwub Yang, Guangzhong*,c (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) Abstract 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 a