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

被引：49

作者：

Li, JJ

Carson, KG

Trivedi, BK

Yue, WS

Ye, Q

Glynn, RA

Miller, SR

Connor, DT

Roth, BD

Luly, JR

Low, JE

Heilig, DJ

Yang, WX

Qin, SX

Hunt, S

机构：

[1] Pfizer Global R&D, Dept Chem, Ann Arbor, MI 48105 USA

[2] Pfizer Global R&D, Dept Biol Mol, Ann Arbor, MI 48105 USA

[3] Millenium Pharmaceut, Dept Chem, Cambridge, MA 02139 USA

[4] Millenium Pharmaceut, Inflammat Biol Dept, Cambridge, MA 02139 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 17期

关键词：

D O I：

10.1016/S0968-0896(03)00399-7

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：3777 / 3790

页数：14

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