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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-D Korean Chemical Society 2006 Bulletin of the Korean Chemical Society Vol.27 No.6
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.