期刊
MOLECULES
卷 17, 期 8, 页码 9961-9970出版社
MDPI AG
DOI: 10.3390/molecules17089961
关键词
CC chemokine receptor 4 (CCR4) antagonists; CKLF1; TARC; MDC; inflammatory disease
资金
- National Natural Science Foundation of China [90813025]
- National Science and Technology Major Project of China [2012ZX09301003]
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.
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