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学科主题: 基础医学
题名:
Design and Synthesis of a Series of Pyrido[2,3-d]pyrimidine Derivatives as CCR4 Antagonists
作者: 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
发表日期: 2012-08-01
DOI: 10.3390/molecules17089961
卷: 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
所属项目编号: 90813025 ; 2012ZX09301003
项目资助者: National Natural Science Foundation of China ; National Science and Technology Major Project of China
WOS记录号: WOS:000308211100092
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/55476
Appears in Collections:基础医学院_期刊论文

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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

Recommended Citation:
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.
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