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

doi:10.6023/cjoc201405018

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

Notes

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

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,yanggz888@126.com E-mail:yanggz888@126.com
基金资助:
中央高校基本科研业务费专项资金(No.CZY13004)资助项目.

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

Chen Yu^a, Bai Shun^a, He Hongwu^b, 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

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).

1. Synthesis and Antitumor Activity Evaluation of Novel Tetrahydro-[4,5]benzothieno[2,3-d]pyrimidinone Derivatives.PDF(1733KB)

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 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

Cite this article

Chen Yu, Bai Shun, He Hongwu, Yang Guangzhong. Synthesis and Antitumor Activity Evaluation of Novel Tetrahydro-[4,5]benzothieno[2,3-d]pyrimidinone Derivatives[J]. Chin. J. Org. Chem., 2014, 34(11): 2362-2369.

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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

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

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