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Design, structure–a...
Design, structure–activity relationships, and enzyme kinetic studies of tricyclic and tetracyclic coumarin–based sulfamates as steroid sulfatase inhibitors
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Chiu, Pei-Fang (author)
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Lin, I-Chun (author)
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Lu, Yeh-Lin (author)
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Chang, Chiao-Nien (author)
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Chan, Hui-Yu (author)
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Lin, Tzung-Shen (author)
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Tsai, Keng-Chang (author)
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- Hsieh, Yves S. Y. (author)
- KTH,Glykovetenskap,School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei 11031, Taiwan
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Chen, Mei-Jou (author)
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Lin, Mei-Hsiang (author)
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Liang, Pi-Hui (author)
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(creator_code:org_t)
- Elsevier BV, 2023
- 2023
- English.
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In: Bioorganic chemistry. - : Elsevier BV. - 0045-2068. ; 138, s. 106581-106581
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- Inhibition of steroid sulfatase (STS) decreases estrogen production and thus, suppresses tumor proliferation. Inspired by irosustat, the first STS inhibitor in clinical trials, we explored twenty-one tricyclic and tetra-heterocyclic coumarin–based derivatives. Their STS enzyme kinetic parameters, docking models, and cytotoxicity toward breast cancer and normal cells were evaluated. Tricyclic derivative 9e and tetracyclic derivative 10c were the most promising irreversible inhibitors developed in this study, with KI of 0.05 and 0.4 nM, and kinact/KI ratios of 28.6 and 19.1 nM−1min−1 on human placenta STS, respectively.
Subject headings
- NATURVETENSKAP -- Kemi -- Organisk kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences -- Organic Chemistry (hsv//eng)
Publication and Content Type
- ref (subject category)
- art (subject category)
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- By the author/editor
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Chiu, Pei-Fang
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Lin, I-Chun
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Lu, Yeh-Lin
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Chang, Chiao-Nie ...
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Chan, Hui-Yu
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Lin, Tzung-Shen
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show more...
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Tsai, Keng-Chang
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Hsieh, Yves S. Y ...
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Chen, Mei-Jou
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Lin, Mei-Hsiang
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Liang, Pi-Hui
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show less...
- About the subject
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- NATURAL SCIENCES
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NATURAL SCIENCES
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and Chemical Science ...
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and Organic Chemistr ...
- Articles in the publication
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Bioorganic chemi ...
- By the university
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Royal Institute of Technology