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 |
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Hauptverfasser: | , , , , , , , , , , , , , |
Format: | Artikel |
Sprache: | kor |
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Zusammenfassung: | 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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ISSN: | 0253-2964 1229-5949 |