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Note | Regular issue | Vol 78, No. 1, 2009, pp.207-212
Published online, 4th September, 2008
DOI: 10.3987/COM-08-11517
First Synthesis of Racemic Methylophiopogonanone B and Its Inhibitory Activity of Hypoxia-inducible Factor-1α

Mikio Fujii, Kiyoshi Egawa, Yasuaki Hirai, Masato Kondo, Hiroyuki Akita, Kiyoshi Nose, Kazuo Toriizuka, and Yoshiteru Ida*

*School of Pharmaceutical Sciences, Toho University, 2-2-1, Miyama, Funabashi, Chiba 274-8510, Japan

Abstract

Methylophiopogonanone B, a constituent of Ophiopogonis tuber, found to be a potent inhibitor of hypoxia induced factor-1α (HIF-1α) activity, was synthesized from 2,4,6-trihydroxy-3,5-dimethylacetophenone in 57% yield. The synthetic methylophiopogonanone B inhibited the reporter activity at 3 to 10 μg/mL.