Title of article :
Chromen-based TNF-α converting enzyme (TACE) inhibitors: Design, synthesis, and biological evaluation Original Research Article
Author/Authors :
Kwangwoo Chun، نويسنده , , Song Kyu Park، نويسنده , , Hwan-Mook Kim، نويسنده , , Yongseok Choi، نويسنده , , Myung-Hwa Kim، نويسنده , , Chun-Ho Park، نويسنده , , Bo-Young Joe، نويسنده , , Tae Gyu Chun، نويسنده , , Hyun-Moo Choi، نويسنده , , Hee-Yoon Lee، نويسنده , , Sung Hee Hong، نويسنده , , Myung Sook Kim، نويسنده , , Ky-Youb Nam، نويسنده , , Gyoonhee Han، نويسنده ,
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.
Keywords :
Rheumatoid arthritis (RA) , Gelastatin hydroxamates , Coumarin derivatives , Metalloproteinase-2 (MMP-2) , Metalloproteinase-9 (MMP-9) , TNF-? converting enzyme (TACE)
