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Design and synthesis of a series of pyrido[2,3-d]pyrimidine derivatives as CCR4 antagonists
Gong H.1; Qi H.2; Sun W.1; Zhang Y.2; Jiang D.3; Xiao J.3; Yang X.1; Wang Y.2; Li S.3
2012-08-01
Source PublicationMolecules
ISSN14203049
Volume17Issue:8Pages:9961-9970
AbstractA 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 LD of compound 6b is 175 mg/kg and the oral LD is greater than 2,000 mg/kg.
KeywordCC chemokine receptor 4 (CCR4) antagonists CKLF1 Inflammatory disease MDC TARC
DOI10.3390/molecules17089961
URLView the original
Language英語
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Cited Times [WOS]:10   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Affiliation1.Jilin University
2.School of Basic Medical Sciences
3.Beijing Institute of Pharmacology and Toxicology
Recommended Citation
GB/T 7714
Gong H.,Qi H.,Sun W.,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 H..,Qi H..,Sun W..,Zhang Y..,Jiang D..,...&Li S..(2012).Design and synthesis of a series of pyrido[2,3-d]pyrimidine derivatives as CCR4 antagonists.Molecules,17(8),9961-9970.
MLA Gong H.,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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