Synthesis and cytotoxicity of 8-cyano-3-substitutedalkyl-5-methyl-4-methylene-7-methoxy-3,4-dihydropyrido[4,3-d]pyrimidines

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成果类型：

期刊论文

作者：

Mo, Wen-Yan;Liang, Yong-Ju;Gu, Yu-Cheng;Fu, Li-Wu*;He, Hong-Wu

通讯作者：

Fu, Li-Wu

作者机构：

[Mo, Wen-Yan; He, Hong-Wu; Gu, Yu-Cheng] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Sch Chem, Wuhan 430079, Peoples R China.

[Fu, Li-Wu; Liang, Yong-Ju] Sun Yat Sen Univ, State Key Lab Oncol S China, Ctr Canc, Guangzhou 510060, Guangdong, Peoples R China.

[Gu, Yu-Cheng] Syngenta, Jealotts Hill Int Res Ctr, Bracknell RG42 6EY, Berks, England.

通讯机构：

[Fu, Li-Wu] S

Sun Yat Sen Univ, State Key Lab Oncol S China, Ctr Canc, Guangzhou 510060, Guangdong, Peoples R China.

语种：

英文

关键词：

Antitumor activity;MTT;Pyrido[4,3-d]pyrimidine;Synthesis

期刊：

Bioorganic & Medicinal Chemistry Letters

ISSN：

0960-894X

年：

2011

卷：

期：

页码：

5975-5977

DOI：

10.1016/j.bmcl.2011.07.067

基金类别：

National Basic Research Program of ChinaNational Basic Research Program of China [2010CB126100]; National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [20772042, 21002037]; 863 ProjectNational High Technology Research and Development Program of China [2006AA09Z419]; Syngenta Ltd; PCSIRTProgram for Changjiang Scholars & Innovative Research Team in University (PCSIRT) [IRT0953]

机构署名：

本校为第一机构

院系归属：

化学学院

摘要：

Synthesis and cytotoxicity of 11 4-methylene pyrido[4,3-d]pyrimidines 5a-k were described. Cytotoxicity assay results showed that some compounds had much stronger antitumor activity than Fluorouracil against KB cell lines. The most active compound 5i exhibited high potency against KB, CNE2, MGC-803 cell lines with IC 50 values of 0.48, 0.15, 0.59 μM, respectively. The preliminary structure-activity relationships indicated that the introduction of benzyl groups bearing electron-donating function groups is favorable ...

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Synthesis and cytotoxicity of 8-cyano-3-substitutedalkyl-5-methyl-4-methylene-7-methoxy-3,4-dihydropyrido[4,3-d]pyrimidines

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