153774-24-4Relevant articles and documents
Design and synthesis of α-ketoamides as cathepsin s inhibitors with potential applications against tumor invasion and angiogenesis
Chen, Jo-Chun,Uang, Biing-Jiun,Lyu, Ping-Chiang,Chang, Jang-Yang,Liu, Ko-Jiunn,Kuo, Ching-Chuan,Hsieh, Hsing-Pang,Wang, Hsin-Chieh,Cheng, Chao-Sheng,Chang, Yi-Hsun,Chang, Margaret Dah-Tsyr,Chang, Wun-Shaing Wayne,Lin, Chun-Cheng
scheme or table, p. 4545 - 4549 (2010/08/19)
A series of small molecules bearing an α-ketoamide warhead were synthesized and evaluated for their ability to inhibit cathepsin S, a key proteolytic enzyme upregulated in many cancers during tumor progression and metastasis. Most of the synthetic compounds were noncytotoxic, but several robustly inhibited cathepsin S (IC50 10 nM) and potently suppressed cell migration, invasion, and capillary tube formation. These results highlight the potential of α-ketoamide therapy for preventing or delaying cancer spread.
