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- Title
Discovery of a Novel 2,6-Difunctionalized 2H-Benzopyran Inhibitors Toward Sphingosylphosphorylcholine Synthetic Pathway as New Anti-inflammatory Target.
- Authors
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
- 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 (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.
- Subjects
CHEMICAL inhibitors; BENZOPYRANS; CHEMICAL synthesis; ANTI-inflammatory agents; CELL proliferation
- Publication
Bulletin of the Korean Chemical Society, 2014, Vol 35, Issue 8, p2385
- ISSN
0253-2964
- Publication type
Article
- DOI
10.5012/bkcs.2014.35.8.2385