Synthesis of pyridine derivatives as potential antagonists of chemokine receptor type 4.
Synthesis of pyridine derivatives as potential antagonists of chemokine receptor type 4.
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DOI：
10.1515/hc-2014-0041
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发表时间：
2014-05
影响因子：
2.3
通讯作者：
Shim H
中科院分区：
文献类型：
--
作者：
Mooring SR;Gaines T;Liang Z;Shim H
合成了一系列吡啶衍生物作为趋化因子受体 4 型的潜在抑制剂。这种趋化因子受体与多种疾病途径有关，包括 HIV-1 增殖、自身免疫性疾病、炎症性疾病和癌症转移。使用亲和结合测定和测试抑制细胞侵袭能力的测定来测试这些化合物的活性。已鉴定出两种命中化合物（2b 和 2j）用于进一步评估，它们可抑制细胞侵袭至少 50%，并且在结合亲和力测定中有效浓度低于 100 nM。合成化合物的结构通过光谱数据得到证实。
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 (2b and 2j) have been identified for further evaluation that inhibit cell invasion by at least 50% and have an effective concentration of less than 100 nM in the binding affinity assay. The structures of the synthesized compounds were confirmed by spectral data.
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