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以氨基酸作为连接臂的聚乙二醇齐墩果酸衍生物及其制备方法和应用
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项目描述
聚乙二醇(PEG)修饰的方法可以用于中药难溶性有效成分前药的合成。PEG作为一种无毒、生物相容性好、无感染和非抗原性的药物载体,常结合水不溶或水溶性低的分子发挥其增溶的作用。氨基酸具有良好的生物相容性和亲和性,且廉价易得,在医药领域发挥着举足轻重的作用,部分抗肿瘤药物经氨基酸修饰...
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2022-05-18
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UPDATE `cms_kjcg` SET `name` = '以氨基酸作为连接臂的聚乙二醇齐墩果酸衍生物及其制备方法和应用' , `sour` = '朝阳龙城科技网' , `read` = 180 , `show` = '/upload/kjcg_62d105e9a3db2.png' , `type` = 16 , `mode` = 3 , `give` = 1 , `info` = '聚乙二醇(PEG)修饰的方法可以用于中药难溶性有效成分前药的合成。PEG作为一种无毒、生物相容性好、无感染和非抗原性的药物载体,常结合水不溶或水溶性低的分子发挥其增溶的作用。氨基酸具有良好的生物相容性和亲和性,且廉价易得,在医药领域发挥着举足轻重的作用,部分抗肿瘤药物经氨基酸修饰后增加了对肿瘤细胞的靶向性,抗肿瘤活性有明显提高,对机体正常细胞的毒性作用也有所降低。 以氨基酸作为连接臂的聚乙二醇齐墩果酸衍生物及其制备方法和应用,涉及一种衍生物及其制备方法和应用,其结构通式为:其中,X=Y=‑CH2或X=H,Y=0,R表示‑H,-CH3,-CH(CH3)2,-CH2CH(CH3)2,-CHCH3(CH2CH3),-CH2C6H5,-(CH2)2-S-CH3;本发明涉及将聚乙二醇通过氨基酸作为连接臂连接到齐墩果酸的C3位羟基,制备了一系列齐墩果酸衍生物,大大提高了齐墩果酸的水溶性。进一步药理活性研究表明此类化合物在抗肿瘤活性等方面大大优于齐墩果酸。本发明的齐墩果酸衍生物以及药物组合物有望开发出抗肿瘤新药。' , `html` = '反应原料易得,反应条件温和,所用溶剂用量少,生成物水溶性提高较大。' , `status` = 2 , `short` = 1652856415 , `addtime` = 1652856415 , `node_id` = 898 , `user_id` = NULL WHERE `id` = 206 [ RunTime:0.000403s ]
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