Discovery of selective and nonpeptidic cathepsin S inhibitors.
Irie, Osamu, Ehara, Takeru, Iwasaki, Atsuko, Yokokawa, Fumiaki, Sakaki, Junichi, Hirao, Hajime, Kanazawa, Takanori, Teno, Naoki, Horiuchi, Miyuki, Umemura, Ichiro, Gunji, Hiroki, Masuya, Keiichi, Hitomi, Yuko, Iwasaki, Genji, Nonomura, Kazuhiko, Tanabe, Keiko, Fukaya, Hiroaki, Kosaka, Takatoshi, Snell, Chris and Hallett, Allan (2008) Discovery of selective and nonpeptidic cathepsin S inhibitors. Bioorganic & Medicinal Chemistry Letters, 18 (14). pp. 3959-3962. ISSN 1464-3405
Abstract
Nonpeptidic, selective, and potent cathepsin S inhibitors were derived from an in-house pyrrolopyrimidine cathepsin K inhibitor by modification of the P2 and P3 moieties. The pyrrolopyrimidine-based inhibitors show nanomolar inhibition of cathepsin S with over 100-fold selectivity against other cysteine proteases, including cathepsin K and L. Some of the inhibitors showed cellular activities in mouse splenocytes as well as oral bioavailabilities in rats.
Item Type: | Article |
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Additional Information: | author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used |
Keywords: | Cathepsin S inhibitor; Pyrrolopyrimidine; Nitrile; Nonpeptidic; Cysteine protease |
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Date Deposited: | 14 Dec 2009 13:53 |
Last Modified: | 31 Jan 2013 01:06 |
URI: | https://oak.novartis.com/id/eprint/803 |