KDR Kinase Inhibitor Isolated from the Mushroom Boletopsis leucomelas.
Three novel p-terphenyl compounds, named boletopsins A (1), B (2), and C (3), and four known analogues (4-7) were isolated from fruiting bodies of the mushroom Boletopsis leucomelas. Compounds 1-7 were tested for KDR kinase inhibitory activity, and boletopsin C (3) was found to have an IC(50) value of 70.7 microM. Compound 3 also showed inhibition of proliferation of human umbilical vein endothelial cells, with an IC(50) value of 9.04 microM.
Kaneko
Akira
A
Department of Pharmacognosy and Phytochemistry, Meiji Pharmaceutical University, Noshio 2-522-1, Kiyose-shi, Tokyo 204-8588, Japan.
Tsukada
Mariko
M
Fukai
Miyuki
M
Suzuki
Toshihiro
T
Nishio
Kazuto
K
Miki
Kazuhiko
K
Kinoshita
Kaoru
K
Takahashi
Kunio
K
Koyama
Kiyotaka
K
D000363:Agaricales / Q000737:chemistry*; D042783:Endothelial Cells / Q000187:drug effects; D048690:Fruiting Bodies, Fungal / Q000737:chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D007564:Japan; D015394:Molecular Structure; D013730:Terphenyl Compounds / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D014471:Umbilical Veins / Q000166:cytology / Q000187:drug effects; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors*
D013730:Terphenyl Compounds; C550056:boletopsin A; C550057:boletopsin B; C550058:boletopsin C; D040301:Vascular Endothelial Growth Factor Receptor-2