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

doi:10.1021/jm100089e

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: 雜誌貢獻 › 文章 › 同行評審

60 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	英語
頁（從 - 到）	4545-4549
頁數	5
期刊	Journal of Medicinal Chemistry
卷	53
發行號	11
DOIs	https://doi.org/10.1021/jm100089e
出版狀態	已發佈 - 6月 2010
對外發佈	是

ASJC Scopus subject areas

分子醫學
藥物發現

UN SDG

此研究成果有助於以下永續發展目標

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10.1021/jm100089e

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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

Chen, JC, Uang, BJ, Lyu, PC, Chang, JY, Liu, KJ, Kuo, CC, Hsieh, HP, Wang, HC, Cheng, CS, Chang, YH, Chang, MDT, Chang, WSW & Lin, CC 2010, 'Design and synthesis of α-ketoamides as cathepsin s inhibitors with potential applications against tumor invasion and angiogenesis', Journal of Medicinal Chemistry, 卷 53, 編號 11, 頁 4545-4549. https://doi.org/10.1021/jm100089e

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abstract = "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.",

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

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doi = "10.1021/jm100089e",

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AU - Chen, Jo Chun

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AU - Chang, Jang Yang

AU - Liu, Ko Jiunn

AU - Kuo, Ching Chuan

AU - Hsieh, Hsing Pang

AU - Wang, Hsin Chieh

AU - Cheng, Chao Sheng

AU - Chang, Yi Hsun

AU - Chang, Margaret Dah Tsyr

AU - Chang, Wun Shaing Wayne

AU - Lin, Chun Cheng

PY - 2010/6

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AB - 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.

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

摘要

ASJC Scopus subject areas

UN SDG

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指紋

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