Synthesis and Cytotoxicity of Novel Diaryl Ureas Containing 2-Amino-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidinyl Group

高等学校化学研究 ›› 2010, Vol. 26 ›› Issue (4): 558-562.

Synthesis and Cytotoxicity of Novel Diaryl Ureas Containing 2-Amino-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidinyl Group

YAO Peng, XUE Hao, LIU Qian, LIU Hong-tao, CHEN Ming-jia and GONG Ping*

Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China.

收稿日期:2009-09-21 修回日期:2009-12-15 出版日期:2010-07-25 发布日期:2010-10-01
通讯作者: GONG Ping. E-mail: gongpinggp@126.com

Synthesis and Cytotoxicity of Novel Diaryl Ureas Containing 2-Amino-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidinyl Group

YAO Peng, XUE Hao, LIU Qian, LIU Hong-tao, CHEN Ming-jia and GONG Ping*

Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China.

Received:2009-09-21 Revised:2009-12-15 Online:2010-07-25 Published:2010-10-01
Contact: GONG Ping. E-mail: gongpinggp@126.com

摘要/Abstract

摘要：

A series of 2-amino-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidinyl substituted diaryl urea derivatives was designed and synthesized. Their in vitro cytotoxicities against two cancer cell lines(Bel-7402 and A549) were evaluated by standard MTT assay. Six of tested compounds 6, 8, 10, 17, 21 and 22 exhibited more potent cytotoxicity superior to sorafenib. The structure activity relationship(SAR) study indicates that 2-amino-5,6,7,8-tetrahydropyrido- [4,3-d]pyrimidinyl group was an option for cytotoxic potency.

关键词: Diaryl urea; 2-Amino-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine; Cytotoxicity, Diaryl urea; 2-Amino-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine; Cytotoxicity, Diaryl urea, 2-Amino-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine, Cytotoxicity

Abstract:

Key words: Diaryl urea, 2-Amino-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine, Cytotoxicity

YAO Peng, XUE Hao, LIU Qian, LIU Hong-tao, CHEN Ming-jia and GONG Ping*. Synthesis and Cytotoxicity of Novel Diaryl Ureas Containing 2-Amino-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidinyl Group[J]. 高等学校化学研究, 2010, 26(4): 558-562.

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Synthesis and Cytotoxicity of Novel Diaryl Ureas Containing 2-Amino-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidinyl Group

Synthesis and Cytotoxicity of Novel Diaryl Ureas Containing 2-Amino-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidinyl Group

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