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초록
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.
키워드
Sphingosylphosphorylcholine; Anti-inflammatory inhibitors; Drug-like library; 2H-benzopyran; Small molecules; PHASE PARALLEL SYNTHESIS; N-ACYL LINKAGE; ATOPIC-DERMATITIS; EXPRESSION; GLUCOSYLCERAMIDE; DERIVATIVES; DEACYLASE; LIBRARY; ENZYME; CELLS
- 제목
- Discovery of a Novel 2,6-Difunctionalized 2H-Senzopyran Inhibitors Toward Sphingosylphosphorylcholine Synthetic Pathway as New Anti-inflammatory Target
- 저자
- 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
- 발행일
- 2014-08-20
- 유형
- Article
- 권
- 35
- 호
- 8
- 페이지
- 2385 ~ 2390