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http://dx.doi.org/10.5012/bkcs.2014.35.8.2385

Discovery of a Novel 2,6-Difunctionalized 2H-Benzopyran Inhibitors Toward Sphingosylphosphorylcholine Synthetic Pathway as New Anti-inflammatory Target  

Lee, Gee-Hyung (Innovative Drug Library Research Center, Science College, Dongguk University)
Lee, Seong Jin (Pharmacology Research Center, Drug Discovery Division, Korea Research Institute of Chemical Technology)
Jeong, Dae Young (Pharmacology Research Center, Drug Discovery Division, Korea Research Institute of Chemical Technology)
Kim, Ha-Young (Innovative Drug Library Research Center, Science College, Dongguk University)
Lee, Doohyun (College of Pharmacy, Research Institute of Pharmaceutical Sciences, Kyungpook National University)
Lee, Taeho (College of Pharmacy, Research Institute of Pharmaceutical Sciences, Kyungpook National University)
Hwang, Jong-Yeon (Pharmacology Research Center, Drug Discovery Division, Korea Research Institute of Chemical Technology)
Park, Woo Kyu (Pharmacology Research Center, Drug Discovery Division, Korea Research Institute of Chemical Technology)
Kong, Jae-Yang (College of Pharmacy, Research Institute of Pharmaceutical Sciences, Keimyung University)
Cho, Heeyeong (Pharmacology Research Center, Drug Discovery Division, Korea Research Institute of Chemical Technology)
Gong, Young-Dae (Innovative Drug Library Research Center, Science College, Dongguk University)
Publication Information
Bulletin of the Korean Chemical Society / v.35, no.8, 2014 , pp. 2385-2390 More about this Journal
Abstract
Novel 2,6-difuctionalized 2H-benzopyrans were synthesized and evaluated for a sphingosylphosphorylcholine(SPC) inhibitor. The synthetic 2H-benzopyrans 1c and 3a showed high potency in SPC-induced cell proliferation assay ($IC_{50}$ < 20 nM). Neither hERG $K^+$ channel binding (> $10{\mu}M$) nor CYP inhibitions (> $10{\mu}M$) were observed. Also, the simple structure-activity relationship (SAR) results were obtained from analysis of 2H-benzopyran derivatives 1-3 and the anti-SPC effect of 2H-benzopyran 1c was confirmed by a HUVEC tube formation assay.
Keywords
Sphingosylphosphorylcholine; Anti-inflammatory inhibitors; Drug-like library; 2H-benzopyran; Small molecules;
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