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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 35, Number 8
BKCSDE 35(8)
August 20, 2014 

Discovery of a Novel 2,6-Difunctionalized 2H-Benzopyran Inhibitors Toward Sphingosylphosphorylcholine Synthetic Pathway as New Anti-inflammatory Target
Gee-Hyung Lee, Seong Jin Lee, Dae Young Jeong, Ha-Young Kim, Doohyun Lee, Taeho Lee, Jong-Yeon Hwang, Woo Kyu Park, Jae-Yang Kong, Heeyeong Cho*, Young-Dae Gong*
Sphingosylphosphorylcholine, Anti-inflammatory inhibitors, Drug-like library, 2H-benzopyran, Small molecules
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 (IC50 < 20 nM). Neither hERG K+ channel binding (> 10 μM) nor CYP inhibitions (> 10 μM) 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.
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