Parallel approach for solution-phase synthesis of 2-quinoxalinol analogues and their inhibition of LPS-induced TNF-alpha release on mouse macrophages in vitro

Liang Zhang; Gang Liu; Suo-De Zhang; Hong-Zhen Yang; Li Li; Xiang-Hong Wu; Junli Yu; Bin-Bin Kou; Song Xu; Jing Li; Gang-Chun Sun; Ya-Fei Ji; Gui-Fang Cheng

doi:10.1021/cc034035h

Parallel approach for solution-phase synthesis of 2-quinoxalinol analogues and their inhibition of LPS-induced TNF-alpha release on mouse macrophages in vitro

J Comb Chem. 2004 May-Jun;6(3):431-6. doi: 10.1021/cc034035h.

Authors

Liang Zhang¹, Gang Liu, Suo-De Zhang, Hong-Zhen Yang, Li Li, Xiang-Hong Wu, Junli Yu, Bin-Bin Kou, Song Xu, Jing Li, Gang-Chun Sun, Ya-Fei Ji, Gui-Fang Cheng

Affiliation

¹ Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, P. R. China.

PMID: 15132605
DOI: 10.1021/cc034035h

Abstract

A parallel solution-phase synthesis of 2-quinoxalinol analogues is described. The key step-simultaneous reductions of m-Ar(NO2)2 to m-Ar(NH2)2 was investigated extensively. We obtained preliminary pharmacological activity of those analogues for the inhibition of LPS-induced TNF-alpha release on mouse macrophage in vitro. Two compounds revealed inhibitory activity, with IC50 values of 0.40 microM (7-amino-6-[(3-methoxypropyl)amino]-3-methyl-2-quinoxalinol) and 2.2 microM (7-amino-6-[(3-butoxypropyl)amino]-3-methyl-2-quinoxalinol), respectively.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Lipopolysaccharides
Macrophages
Mice
Pharmaceutical Solutions*
Solutions
Tumor Necrosis Factor-alpha*

Substances

Lipopolysaccharides
Pharmaceutical Solutions
Solutions
Tumor Necrosis Factor-alpha