申请人:Tianjin Hemey Bio-Tech Co., Ltd.
公开号:EP2123283A1
公开(公告)日:2009-11-25
The present invention provides aminoside tetracyclic anthraquinones represented by formula (I) or formula (II), wherein the piptides are introduced to connect tetracyclic anthraquinones and fatty acid saturated or unsaturated in order to make the anticancer agents to be absorbed and released selectively; meanwhile some water-solubility groups are also introduced into the branched chain, aminosaccharide and tetracyclic moiety of the compounds to improve the water-solubility. The present invention also provides the preparative method and the use thereof as pharmaceutically active components for treating the diseases cured by aminoside tetracyclic anthraquinone, for example cancer, such as intestines, liver, gastric, breast, lung, ovary, prostate, brain glioma, lymph, skin, pigment, thyroid gland, multiple bone marrow cancer and leukemia.
本发明提供了以式(I)或式(II)为代表的氨基苷类四环蒽醌,其中引入了肽类连接四环蒽醌和饱和或不饱和脂肪酸,以使抗癌剂被选择性吸收和释放;同时在化合物的支链、氨基糖和四环分子中还引入了一些水溶性基团,以提高水溶性。本发明还提供了制备方法及其作为药物活性成分的用途,用于治疗氨基苷类四环蒽醌可治愈的疾病,例如癌症,如肠癌、肝癌、胃癌、乳腺癌、肺癌、卵巢癌、前列腺癌、脑胶质瘤、淋巴癌、皮肤癌、色素癌、甲状腺癌、多发性骨髓癌和白血病等。