abstract |
Hypericin, helianthrone and derivatives thereof of general formula (I) wherein the dotted line between positions 11 and 12 represents an optional C11-C12 bond; R is selected from the group consisting of hydroxy, C1-C10 alkoxy, NH-C1-C10 alkyl, and NH-hydroxy(C1-C10)alkyl but R is H at positions 8 and 15 when there is no C11-C12 bond; R' is selected from the group consisting of hydroxy and C1-C10 alkoxy; and R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen, hydroxy, chloro, bromo, C1-C10 alkyl, C1-C10 alkoxy, and C1-C10 alkoxycarbonyl, are useful as inhibitors of angiogenesis and can be used to prevent formation of metastases and restenosis and for the treatment of angiogenesis-associated ophthalmologic disorders. In addition, the helianthrones of formula (I) can be used for the treatment of tumors in the absence of light irradiation. |