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Note | Regular issue | Vol 78, No. 8, 2009, pp.2061-2065
Published online, 14th April, 2009
DOI: 10.3987/COM-09-11684
Dihydrochalcone Designed from Methylophiopogonanone B Strongly Inhibits Hypoxia-inducible Factor (HIF)-1α Activity

Mikio Fujii,* Kiyoshi Egawa, Yasuaki Hirai, Masato Kondo, Kotaro Fujii, Hidehiro Uekusa, 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

Inhibition of hypoxia-inducible factor (HIF)-1α activity of methylophiopogonanone B (1) and its derivatives were investigated. As the modification of the structure of 1, dihydrochalcone (11) was leaded and showed one order higher activity (IC50: 0.2 μg/mL) than methylophiopogonanone B (1) (IC50: 2.2 μg/mL).