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学科主题基础医学
Design and Synthesis of a Series of Pyrido[2,3-d]pyrimidine Derivatives as CCR4 Antagonists
Gong, Hongwei1,2,3; Qi, Hui4; Sun, Wei2; Zhang, Yang4; Jiang, Dan1; Xiao, Junhai1; Yang, Xiaohong2; Wang, Ying4; Li, Song1
关键词Cc Chemokine Receptor 4 (Ccr4) Antagonists Cklf1 Tarc Mdc Inflammatory Disease
刊名MOLECULES
2012-08-01
DOI10.3390/molecules17089961
17期:8页:9961-9970
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Organic
研究领域[WOS]Chemistry
关键词[WOS]CHEMOKINE-LIKE FACTOR-1 ; AIRWAY INFLAMMATION ; OPTIMIZATION ; POTENT ; CONTRIBUTES ; EXPLORATION ; THYMUS ; AGENTS ; CELLS ; MICE
英文摘要

A series of pyrido[2,3-d]pyrimidine derivatives were designed and synthesized based on known CC chemokine receptor 4 (CCR4) antagonists. The activities of all the newly synthesized compounds were evaluated using a chemotaxis inhibition assay. Compound 6b was proven to be a potent CCR4 antagonist that can block cell chemotaxis induced by macrophage-derived chemokine (MDC), thymus and activation regulated chemokine (TARC), and CKLF1, the natural ligands of CCR4. In addition, compound 6b is more effective than budesonide in the murine rhinitis model. The intravenous injection LD50 of compound 6b is 175 mg/kg and the oral LD50 is greater than 2,000 mg/kg.

语种英语
WOS记录号WOS:000308211100092
项目编号90813025 ; 2012ZX09301003
资助机构National Natural Science Foundation of China ; National Science and Technology Major Project of China
引用统计
被引频次:10[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/55476
专题北京大学基础医学院
作者单位1.Jilin Univ, Sch Publ Hlth, Changchun 130021, Peoples R China
2.Beijing Inst Pharmacol & Toxicol, Lab Comp Aided Drug Design & Discovery, Beijing 100850, Peoples R China
3.Jilin Univ, Sch Pharmaceut Sci, Changchun 130021, Peoples R China
4.Peking Univ, Hlth Sci Ctr, Sch Basic Med Sci, Dept Immunol,Key Lab Med Immunol,Minist Hlth, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Gong, Hongwei,Qi, Hui,Sun, Wei,et al. Design and Synthesis of a Series of Pyrido[2,3-d]pyrimidine Derivatives as CCR4 Antagonists[J]. MOLECULES,2012,17(8):9961-9970.
APA Gong, Hongwei.,Qi, Hui.,Sun, Wei.,Zhang, Yang.,Jiang, Dan.,...&Li, Song.(2012).Design and Synthesis of a Series of Pyrido[2,3-d]pyrimidine Derivatives as CCR4 Antagonists.MOLECULES,17(8),9961-9970.
MLA Gong, Hongwei,et al."Design and Synthesis of a Series of Pyrido[2,3-d]pyrimidine Derivatives as CCR4 Antagonists".MOLECULES 17.8(2012):9961-9970.
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