Novel Inhibitors of Prolyl 4-Hydroxylase; Solid-phase Synthesis of 2,2-Dimethyl-3,4-Dialkoxy-Substituted 6-Aminobenzopyran Derivatives

2,2-Dimethyl-3,4-dialkoxy-substituted 6-aminobenzopyran analogues (eg., 7 and 8) were identified as prolyl 4-hydroxylase inhibitors via a screening process using HSC-T6 and LI 90 cells that express an immortalized rat hepatic stellate cell line and as part of a test of the type I collagen contents e...

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Veröffentlicht in:Bulletin of the Korean Chemical Society 2006, Vol.27 (6), p.909-917
Hauptverfasser: Seo, Jin-soo, Joo, Yang-Hee, Yi, Jung-Bum, Lee, Eun-Ju, Lee, Nam-Kyu, Cho, Yong-Balk, Kwak, Wie-Jong, Hwang, Jong-Yeon, Jeon, Yong-Seog, Jeon, Hyun-Suk, Yoo, Sung-eun, Yoon, Cheol-Min, Dong, Mi-Sook, Gong, Young-Dae
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container_issue 6
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container_title Bulletin of the Korean Chemical Society
container_volume 27
creator Seo, Jin-soo
Joo, Yang-Hee
Yi, Jung-Bum
Lee, Eun-Ju
Lee, Nam-Kyu
Cho, Yong-Balk
Kwak, Wie-Jong
Hwang, Jong-Yeon
Jeon, Yong-Seog
Jeon, Hyun-Suk
Yoo, Sung-eun
Yoon, Cheol-Min
Dong, Mi-Sook
Gong, Young-Dae
description 2,2-Dimethyl-3,4-dialkoxy-substituted 6-aminobenzopyran analogues (eg., 7 and 8) were identified as prolyl 4-hydroxylase inhibitors via a screening process using HSC-T6 and LI 90 cells that express an immortalized rat hepatic stellate cell line and as part of a test of the type I collagen contents employing the ELISA method. A subsequent lead optimization effort based on solid-phase parallel synthesis led to the identification of 2,2-dimethyl-3,4-dialkoxy-substituted 6-aminobenzopyrans as potent inhibitors of prolyl 4-hydroxylase.
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title Novel Inhibitors of Prolyl 4-Hydroxylase; Solid-phase Synthesis of 2,2-Dimethyl-3,4-Dialkoxy-Substituted 6-Aminobenzopyran Derivatives
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