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Title 

Chromen-based TNF-α converting enzyme (TACE) inhibitors: Design, synthesis, and biological evaluation

Authors 

K ChunSong Kyu ParkHwan Mook KimY ChoiM H KimC H ParkB Y JoeT G ChunH M ChoiH Y LeeS H HongM S KimK Y NamG Han

Publisher 

Elsevier

Issue Date 

2008

Citation 

Bioorganic & Medicinal Chemistry, vol. 16, no. 1, pp. 530-535

Keywords 

coumarin derivativesgelastatin hydroxamatesmetalloproteinase-2 (MMP-2)metalloproteinase-9 (MMP-9)rheumatoid arthritis (RA)TNF-α converting enzyme (TACE)chromene derivativematrix metalloproteinase inhibitorn hydroxy 2 methyl 3 (6 methyl 2 oxo 2h chromen 3 yl)propionamidetumor necrosis factor alpha converting enzyme

Abstract 

A series of coumarin types MMP inhibitors were designed based on gelastatin hydroxamates (1) and evaluated for TACE, cellular TNF-α, and NO inhibitory activities. Among them, compounds 9b had potent inhibitory activities in enzymatic and cellular assays and good selectivity to MMP-2 and MMP-9. Further investigation of 9b will be carried out for its efficacy in RA animal model system.

ISSN 

0968-0896

Link 

http://dx.doi.org/10.1016/j.bmc.2007.09.014

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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