Synthesis and peptidyl-prolyl isomerase inhibitory activity of quinoxalines as ligands of cyclophilin A

Feng Wang; Jing Chen; Xuejun Liu; Xu Shen; Xuchang He; Hualiang Jiang; Donglu Bai

doi:10.1248/cpb.54.372

Synthesis and peptidyl-prolyl isomerase inhibitory activity of quinoxalines as ligands of cyclophilin A

Chem Pharm Bull (Tokyo). 2006 Mar;54(3):372-6. doi: 10.1248/cpb.54.372.

Authors

Feng Wang¹, Jing Chen, Xuejun Liu, Xu Shen, Xuchang He, Hualiang Jiang, Donglu Bai

Affiliation

¹ Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, China.

PMID: 16508195
DOI: 10.1248/cpb.54.372

Abstract

In search of small molecule compounds as the ligands of cyclophilin A, a series of quinoxalines were prepared, and their K(d) values of cyclophilin A and IC50 values for peptidyl-prolyl isomerase activity of cyclophilin A were tested. The results suggest that some quinoxalines are promising ligands of cyclophilin A.

MeSH terms

Cyclophilin A / chemistry*
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / pharmacology*
Indicators and Reagents
Kinetics
Magnetic Resonance Spectroscopy
Peptidylprolyl Isomerase / antagonists & inhibitors*
Quinoxalines / chemistry*
Spectrophotometry, Infrared
Structure-Activity Relationship
Surface Plasmon Resonance

Substances

Enzyme Inhibitors
Indicators and Reagents
Quinoxalines
Cyclophilin A
Peptidylprolyl Isomerase