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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 Korean Chemical Society 2014 Bulletin of the Korean Chemical Society Vol.35 No.8
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 ($IC_{50}$ < 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.