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    • 9. 发明授权
    • Anticancer anthraquinones and method of use thereof
    • 抗癌蒽醌类及其使用方法
    • US06875746B1
    • 2005-04-05
    • US10355483
    • 2003-01-31
    • Muraleedharan G. NairRobert H. CichewiczNavindra P. SeeramYanjun Zhang
    • Muraleedharan G. NairRobert H. CichewiczNavindra P. SeeramYanjun Zhang
    • C07H15/244A61K31/122A61K31/21A61K31/70A61K31/704A61P33/10A61P33/12C07C50/34C07C50/38C07C66/02C07C69/157A01N43/04A01N37/00
    • A61K31/70A61K31/21C07C50/38Y02A50/423
    • Anthraquinones are described which have anticancer or antitumor activity and which are useful for inhibiting cancer cells and cells comprising tumors in vitro or in vivo. Preferably, the anthraquinones have the chemical formula: wherein R1 is selected from the group consisting of hydrogen, alkyl, and substituted alkyl; R2 is a group containing 1-12 carbons selected from the group consisting of alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate and combinations thereof; and R3 is a group containing 1 to 12 carbons selected from the group consisting of methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, and combinations thereof. The preferred anthraquinones are 1-hydroxy-2-acetyl-3,6-methyl anthraquinone, 2-acetyl-3,6-methyl anthraquinone monoacetate, 1-hydroxy-2-acetyl-3,7-methyl anthraquinone, 2-acetyl-3,7-methyl anthraquinone monoacetate, 1,2,8-trihydroxy-3-methyl anthraquinone, 1,8-dihydroxy-2-O-β-D-glucopyranoside anthraquinone, 1,2,8-trihydroxy-3-hydroxymethyl anthraquinone, and 1,8-dihydroxy-3-carboxy anthraquinone.
    • 描述了具有抗癌或抗肿瘤活性的蒽醌,其可用于在体外或体内抑制癌细胞和包含肿瘤的细胞。 优选地,蒽醌具有以下化学式:其中R 1选自氢,烷基和取代的烷基; R2是含有选自烷基,取代的烷基,醛,羟基,羟甲基,酸基,碳水化合物及其组合的1-12个碳的基团; 并且R 3是选自甲基,烷基,取代的烷基,醛,羟基,羟甲基,酸基,碳水化合物及其组合中的1至12个碳的基团。 优选的蒽醌是1-羟基-2-乙酰基-3,6-甲基蒽醌,2-乙酰基-3,6-甲基蒽醌单乙酸酯,1-羟基-2-乙酰基-3,7-甲基蒽醌,2-乙酰基 - 3,7-甲基蒽醌单乙酸酯,1,2,8-三羟基-3-甲基蒽醌,1,8-二羟基-2-O-β-D-吡喃葡萄糖苷蒽醌,1,2,8-三羟基-3-羟甲基蒽醌 ,和1,8-二羟基-3-羧基蒽醌。