Li Jie Jack, Carson Kenneth G, Trivedi Bharat K, Yue Wen Song, Ye Qing, Glynn Roberta A, Miller Steven R, Connor David T, Roth Bruce D, Luly Jay R, Low Joseph E, Heilig David J, Yang Weixing, Qin Shixin, Hunt Stephen
Chemistry Department, Pfizer Global R&D, 2800 Plymouth Rd., Ann Arbor, MI 48105, USA.
Bioorg Med Chem. 2003 Aug 15;11(17):3777-90. doi: 10.1016/s0968-0896(03)00399-7.
Interleukin-8 modulation is implicated in many inflammatory and cancer diseases. Starting from a mass-screening hit, the synthesis and structure-activity relationship of 2-amino-3-heteroarylquinoxalines as non-peptide, small molecule interleukine-8 receptor antagonists have been developed. The optimized derivatives, PD 0210293 (13y) and PD 0220245 (13r), show inhibition of both IL-8 receptor binding and IL-8-mediated neutrophil chemotaxis.
白细胞介素-8调节与许多炎症和癌症疾病有关。从一次大规模筛选的活性物质出发，已开发出2-氨基-3-杂芳基喹喔啉作为非肽类小分子白细胞介素-8受体拮抗剂的合成及其构效关系。优化后的衍生物PD 0210293（13y）和PD 0220245（13r）对白细胞介素-8受体结合和白细胞介素-8介导的中性粒细胞趋化作用均有抑制作用。
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