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

Bulletin of the Korean chemical society

Young-Dae Gong¹  Heeyeong Cho¹  Dae Young Jeong¹  Gee-Hyung Lee¹  Taeho Lee¹  Woo Kyu Park¹  Jong-Yeon Hwang¹  Jae-Yang Kong¹  Doohyun Lee¹  Ha-Young Kim¹  Seong Jin Lee¹ 

关键词: Sphingosylphosphorylcholine;    Anti-inflammatory inhibitors;    Drug-like library;    2H-benzopyran;    Small molecules;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

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.

【 授权许可】

Unknown