Document Type
Article
Publication Date
9-23-2010
Publication Title
Journal of Medicinal Chemistry
Volume
53
Issue
18
Pages
6653–6680
Publisher Name
American Chemical Society
Abstract
α-Sulfone-α-piperidine and α-tetrahydropyranyl hydroxamates were explored that are potent inhibitors of MMP’s-2, -9, and -13 that spare MMP-1, with oral efficacy in inhibiting tumor growth in mice and left-ventricular hypertrophy in rats and in the bovine cartilage degradation ex vivo explant system. α-Piperidine 19v (SC-78080/SD-2590) was selected for development toward the initial indication of cancer, while α-piperidine and α-tetrahydropyranyl hydroxamates 19w (SC-77964) and 9i (SC-77774), respectively, were identified as backup compounds.
Recommended Citation
Becker, Daniel P.; Barta, Thomas E.; Bedell, Louis J.; and Boehm, Terri L.. Orally Active MMP-1 Sparing α-tetrahydropyranyl and α-piperidinyl Sulfone Matrix Metalloproteinase (MMP) Inhibitors with Efficacy in Cancer, Arthritis, and Cardiovascular Disease. Journal of Medicinal Chemistry, 53, 18: 6653–6680, 2010. Retrieved from Loyola eCommons, Chemistry: Faculty Publications and Other Works, http://dx.doi.org/10.1021/jm100669j
Creative Commons License
This work is licensed under a Creative Commons Attribution-Noncommercial-No Derivative Works 3.0 License.
Copyright Statement
© 2010 American Chemical Society
Comments
Author Posting © American Chemical Society, 2010. This is the author's version of the work. It is posted here by permission of American Chemical Society for personal use, not for redistribution. The definitive version was published in Journal of Medicinal Chemistry, Volume 53, Issue 18, September 23, 2010. http://dx.doi.org/10.1021/jm100669j