Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1379600 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
Abstract
The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors bearing a butynyloxy P1′ group was explored. In particular, compound 5k has excellent in vitro potency against TACE enzyme and in cells, and oral activity in an in vivo model of TNF-α production and a collagen-induced arthritis model.
Graphical abstractThe SAR of a series of potent sulfonamide hydroxamate TACE inhibitors bearing a butynyloxy P1′ group was explored. In particular, compound 5k has excellent in vitro potency against TACE enzyme and in cells, and oral activity in an in vivo model of TNF-α production and a collagen-induced arthritis model.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
J.I. Levin, J.M. Chen, L.M. Laakso, M. Du, X. Du, A.M. Venkatesan, V. Sandanayaka, A. Zask, J. Xu, W. Xu, Y. Zhang, J.S. Skotnicki,