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.
Bibliographical noteFunding Information:
This research was supported by Seoul R&BD Program (10541), a Grant (0405-NS01-0704-0001) of the Korean Health 21 R&D Project, Ministry of Health and Welfare, and the Brain Korea 21 project the Republic of Korea.
All Science Journal Classification (ASJC) codes
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry