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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 27, Number 6
BKCSDE 27(6)
June 20, 2006 

Novel Inhibitors of Prolyl 4-Hydroxylase; Solid-phase Synthesis of 2,2-Dimethyl-3,4-Dialkoxy-Substituted 6-Aminobenzopyran Derivatives
Jin-soo Seo, Yang-Hee Joo, Jung Bum Yi, Eun Ju Lee, Namkyu Lee, Yong-Balk Cho, Wie Jong Kwak, Jong Yeon Hwang, Yong Seog Jeon, Hyun Suk Jeon, Sung-eun Yoo, Cheol Min Yoon, Mi-Sook Dong*, Young-Dae Gong*
Prolyl 4-hydroxylase, Collagen contents, Solid-phase synthesis, 2,2-Dimethyl-3,4-dialkoxysubstituted 6-aminobenzopyrans
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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