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Ametantrone即1,4-双{2-[2-羟乙基)氨基]乙氨基}-9,10蒽二酮二乙酸盐(NSC—287513)是一个新的氨基蒽醌类衍生物,它是一种深蓝色染料。结构如下:在美国癌症研究所进行的随机筛选中,发现其对小鼠P 388、L 1210白血病,B 16黑色素瘤和结肠癌26等瘤株均有抗肿瘤作用。Ametantrone的作用机制尚未完全阐明。已发现它几可完全阻滞细胞周期的G2期。它的平面醌环具有插入作用,由于可使DNA耐受热变性作用,故可与DNA结合并抑制胸苷和尿苷掺入L 1210细胞中。对P 388白血病的抗蒽环类亚系对ametantrone有抗药性。毒理学试验的初步数据显示,它对心脏的毒性比常
Ametantrone, 1,4-bis {2- [2-hydroxyethyl) amino] ethylamino} -9,10 anthracenedione diacetate (NSC-287513) is a new aminoanthraquinone derivative Is a dark blue dye. The structure is as follows: In the random screening conducted by the American Cancer Institute, it was found to have antitumor effects on tumor cells such as mouse P 388, L 1210 leukemia, B 16 melanoma and colon cancer 26. Ametantrone’s mechanism of action has not yet been fully elucidated. It has been found that it almost completely blocks the G2 phase of the cell cycle. Its planar quinone ring has an insertion effect that binds to DNA and inhibits the incorporation of thymidine and uridine into L1210 cells due to its ability to withstand thermal denaturation. The anti-anthracycline subline of P388 leukemia is resistant to ametantrone. Preliminary data from toxicology tests show that it is more toxic to the heart than usual