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

Autor: Yong-Balk Cho, Eun Ju Lee, Hyun Suk Jeon, Mi-Sook Dong, Yang-Hee Joo, Jung Bum Yi, Jin-soo Seo, Yong Seog Jeon, Cheol Min Yoon, Sung-Eun Yoo, Young-Dae Gong, Jong Yeon Hwang, Namkyu Lee, Wie Jong Kwak
Rok vydání: 2006
Předmět:
Zdroj: Bulletin of the Korean Chemical Society. 27:909-917
ISSN: 0253-2964
DOI: 10.5012/bkcs.2006.27.6.909
Popis: 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.
Databáze: OpenAIRE