Design and synthesis of α-ketoamides as cathepsin s inhibitors with potential applications against tumor invasion and angiogenesis

Jo Chun Chen, Biing Jiun Uang, Ping Chiang Lyu, Jang Yang Chang, Ko Jiunn Liu, Ching Chuan Kuo, Hsing Pang Hsieh, Hsin Chieh Wang, Chao Sheng Cheng, Yi Hsun Chang, Margaret Dah Tsyr Chang, Wun Shaing Wayne Chang, Chun Cheng Lin

研究成果: Article

32 引文 斯高帕斯(Scopus)

摘要

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.

原文English
頁(從 - 到)4545-4549
頁數5
期刊Journal of Medicinal Chemistry
53
發行號11
DOIs
出版狀態Published - 2010 六月 10

    指紋

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

引用此

Chen, J. C., Uang, B. J., Lyu, P. C., Chang, J. Y., Liu, K. J., Kuo, C. C., Hsieh, H. P., Wang, H. C., Cheng, C. S., Chang, Y. H., Chang, M. D. T., Chang, W. S. W., & Lin, C. C. (2010). Design and synthesis of α-ketoamides as cathepsin s inhibitors with potential applications against tumor invasion and angiogenesis. Journal of Medicinal Chemistry, 53(11), 4545-4549. https://doi.org/10.1021/jm100089e