Synthesis and structure–Activity relationship of 2-amino-3-heteroaryl-quinoxalines as non-peptide, small-Molecule antagonists for interleukin-8 receptor

…, WS Yue, Q Ye, RA Glynn, SR Miller, DT Connor…

Index: 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 Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 17 p. 3777 - 3790

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Citation Number: 39

Abstract

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.