Synthesis and structure-activity relationship of 2-amino-3-heteroaryl-quinoxalines as non-peptide,small-molecule antagonists for interleukin-8 receptor |
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| Authors: | 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 |
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| Affiliation: | Chemistry Department, Pfizer Global R&D, 2800 Plymouth Rd., Ann Arbor, MI 48105, USA. jack.li@pfizer.com |
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| 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. |
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