Synthesis of pyridine derivatives as potential antagonists of chemokine receptor type 4

A series of pyridine derivatives were synthesized as potential inhibitors of chemokine receptor type 4. This chemokine receptor has been linked to various disease pathways including HIV-1 proliferation, autoimmune disorders, inflammatory diseases, and cancer metastasis. The compounds were tested for...

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Veröffentlicht in:Heterocyclic communications 2014-06, Vol.20 (3), p.149-153
Hauptverfasser: Mooring, Suazette Reid, Gaines, Theresa, Liang, Zhongxing, Shim, Hyunsuk
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Sprache:eng
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Zusammenfassung:A series of pyridine derivatives were synthesized as potential inhibitors of chemokine receptor type 4. This chemokine receptor has been linked to various disease pathways including HIV-1 proliferation, autoimmune disorders, inflammatory diseases, and cancer metastasis. The compounds were tested for activity using an affinity binding assay and an assay that tests the ability to inhibit cell invasion. Two hit compounds ( and ) have been identified for further evaluation that inhibit cell invasion by at least 50% and have an effective concentration of less than 100 n in the binding affinity assay. The structures of the synthesized compounds were confirmed by spectral data.
ISSN:0793-0283
2191-0197
DOI:10.1515/hc-2014-0041