当前位置: X-MOL 学术Heterocycl. Commun. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis of pyridine derivatives as potential antagonists of chemokine receptor type 4
Heterocyclic Communications ( IF 2.3 ) Pub Date : 2014-01-01 , DOI: 10.1515/hc-2014-0041
Suazette Reid Mooring 1 , Theresa Gaines 1 , Zhongxing Liang 2 , Hyunsuk Shim 2
Affiliation  

Abstract 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.

中文翻译:

合成吡啶衍生物作为 4 型趋化因子受体的潜在拮抗剂

摘要 合成了一系列吡啶衍生物作为 4 型趋化因子受体的潜在抑制剂。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化合物的活性。两种命中化合物(2b 和 2j)已被鉴定用于进一步评估,它们抑制细胞侵袭至少 50%,并且在结合亲和力测定中具有小于 100 nm 的有效浓度。合成化合物的结构由光谱数据证实。
更新日期:2014-01-01
down
wechat
bug