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Discovery of a Novel 2,6-Difunctionalized 2H-Senzopyran Inhibitors Toward Sphingosylphosphorylcholine Synthetic Pathway as New Anti-inflammatory Targetopen access
- Authors
- Lee, Gee-Hyung; Lee, Seong Jin; Jeong, Dae Young; Kim, Ha-Young; Lee, Doohyun; Lee, Taeho; Hwang, Jong-Yeon; Park, Woo Kyu; Kong, Jae-Yang; Cho, Heeyeong; Gong, Young-Dae
- Issue Date
- 20-Aug-2014
- Publisher
- WILEY-V C H VERLAG GMBH
- Keywords
- Sphingosylphosphorylcholine; Anti-inflammatory inhibitors; Drug-like library; 2H-benzopyran; Small molecules
- Citation
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.35, no.8, pp 2385 - 2390
- Pages
- 6
- Indexed
- SCI
SCIE
SCOPUS
KCI
- Journal Title
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- Volume
- 35
- Number
- 8
- Start Page
- 2385
- End Page
- 2390
- ISSN
- 0253-2964
1229-5949
- 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 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.
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