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学科主题基础医学
Design, Synthesis and SAR Study of Novel Trisubstituted Pyrimidine Amide Derivatives as CCR4 Antagonists
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
2014-03-01
DOI10.3390/molecules19033539
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
WOS记录号WOS:000335826800053
项目编号2012AA020301 ; 2012ZX09301003-001-002 ; 2012ZX09301003-003
资助机构National High Technology Research and Development program of China (863 program) ; National Science and Technology Major project
引用统计
被引频次:1[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
版本出版稿
条目标识符http://ir.bjmu.edu.cn/handle/400002259/55743
专题北京大学基础医学院_免疫学系
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
推荐引用方式
GB/T 7714
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.
APA Xu, Libao.,Zhang, Yang.,Dai, Wenjie.,Wang, Ying.,Jiang, Dan.,...&Li, Song.(2014).Design, Synthesis and SAR Study of Novel Trisubstituted Pyrimidine Amide Derivatives as CCR4 Antagonists.MOLECULES,19(3),3539-3551.
MLA Xu, Libao,et al."Design, Synthesis and SAR Study of Novel Trisubstituted Pyrimidine Amide Derivatives as CCR4 Antagonists".MOLECULES 19.3(2014):3539-3551.
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