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

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

ㆍ 저자명: Lee. Gee-Hyung,Lee. Seong Jin,Jeong. Dae Young,Kim. Ha-Young,Lee. Doohyun,Lee. Taeho,Hwang. Jong-Yeon,Park. Woo Kyu,Kong. Jae-Ya
ㆍ 간행물명: Bulletin of the Korean Chemical Society
ㆍ 권/호정보: 2014년|35권 8호|pp.2385-2390 (6 pages)
ㆍ 발행정보: 대한화학회
ㆍ 파일정보: 정기간행물|ENG|
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ㆍ 주제분야: 기타

이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.

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기타언어초록

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.

키워드

Sphingosylphosphorylcholine Anti-inflammatory inhibitors Drug-like library 2H-benzopyran Small molecules

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