S-dimethylarsino-thiosuccinic acid s-dimethylarsino-2-thiobenzoic acid s-(dimethylarsino) glutathione as treatments for cancer
申请人:——
公开号:US20040034095A1
公开(公告)日:2004-02-19
Arsenic trioxide, an inorganic compound, is commercially available anti-cancer agent but it carries significant toxicity. Organic arsenicals, on the other hand, are much less toxic, to the extent that the methylation of inorganic arsenic in vivo into organic arsenicals has been considered a detoxification reaction. New organic arsenic derivatives have been synthesized, including S-dimethylarsino-glutathione, S-dimethylarsino-thiosuccinic acid and S-dimethylarsino-thiobenzoic acid, and established its potent in vitro cytotoxic activity against numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia. Results form a basis for the development of S-dimethylarsino-glutathione, S-dimethylarsino-thiosuccinic acid, S-dimethylarsino-thiobenzoic acid, and other organic arsenicals as an anti-cancer therapy, combining high efficacy with very low, if any, toxicity.
三氧化二砷是一种无机化合物,是一种商业上可获得的抗癌药物,但具有显著的毒性。另一方面,有机砷化合物毒性要小得多,甚至认为体内将无机砷甲基化为有机砷化合物是一种解毒反应。已合成了新的有机砷衍生物,包括S-二甲基砷谷胱甘肽、S-二甲基砷硫代琥珀酸和S-二甲基砷硫代苯甲酸,并确定了它们在体外对多种人类肿瘤细胞系以及对患有白血病的患者的恶性血细胞具有强大的细胞毒活性。这些结果为开发S-二甲基砷谷胱甘肽、S-二甲基砷硫代琥珀酸、S-二甲基砷硫代苯甲酸和其他有机砷化合物作为抗癌疗法提供了基础,结合了高效性和非常低的毒性。