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学科主题: 基础医学
题名:
Design, Synthesis and SAR Study of Novel Trisubstituted Pyrimidine Amide Derivatives as CCR4 Antagonists
作者: Xu, Libao1,2; Zhang, Yang3; Dai, Wenjie4; Wang, Ying3; Jiang, Dan2; Wang, Lili2; Xiao, Junhai2; Yang, Xiaohong1; Li, Song1,2
关键词: antagonists ; pyrimidine amides ; synthesis ; structure-activity relationship
刊名: MOLECULES
发表日期: 2014-03-01
DOI: 10.3390/molecules19033539
卷: 19, 期:3, 页:3539-3551
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 RECEPTORS ; INFLAMMATION ; SERIES ; IDENTIFICATION ; OPTIMIZATION ; EXPRESSION ; TARGETS ; CELLS
英文摘要:

The design, synthesis and structure-activity relationship studies of some novel trisubstituted pyrimidine amide derivatives prepared as CCR4 antagonists are described. The activities of these compounds were evaluated by the CCR4-MDC chemotaxis inhibition assay. Compound 1, which we have previously reported as a potent antagonist of CCR4, was employed as the positive control. The results indicated that most of the synthesized compounds exhibited some chemotaxis inhibition activity against CCR4. Of these new compounds, compounds 6c, 12a and 12b, with IC50 values of 0.064, 0.077 and 0.069 mu M, respectively, showed higher or similar activity compared with compound 1 (IC50 of 0.078 mu M). These compounds provide a basis for further structural modifications. The systematic structure-activity relationship of these trisubstituted pyrimidine amide derivatives was discussed based on the obtained experimental data. The results from the SAR study may be useful for identifying more potent CCR4 antagonists.

语种: 英语
所属项目编号: 2012AA020301 ; 2012ZX09301003-001-002 ; 2012ZX09301003-003
项目资助者: National High Technology Research and Development program of China (863 program) ; National Science and Technology Major project
WOS记录号: WOS:000335826800053
Citation statistics:
内容类型: 期刊论文
版本: 出版稿
URI标识: http://ir.bjmu.edu.cn/handle/400002259/55743
Appears in Collections:基础医学院_免疫学系_期刊论文

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作者单位: 1.Jilin Univ, Sch Pharmaceut Sci, Changchun 130021, Peoples R China
2.Beijing Inst Pharmacol & Toxicol, Lab Comp Aided Drug Design & Discovery, Beijing 100850, Peoples R China
3.Peking Univ, Sch Basic Med Sci, Dept Immunol, Key Lab Med Immunol,Minist Hlth,Hlth Sci Ctr, Beijing 100191, Peoples R China
4.Shenyang Pharmaceut Univ, Shenyang 110016, Peoples R China

Recommended Citation:
Xu, Libao,Zhang, Yang,Dai, Wenjie,et al. Design, Synthesis and SAR Study of Novel Trisubstituted Pyrimidine Amide Derivatives as CCR4 Antagonists[J]. MOLECULES,2014,19(3):3539-3551.
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