用于肿瘤治疗的异喹啉-3-羧酸为药效团的二价态配体

来源 :第十五届胶体与界面化学会议 | 被引量 : 0次 | 上传用户:1010
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自从1974年分离得到具有抗肿瘤活性的四氢异喹啉天然产物naphthriydinomycin起,异喹啉生物碱的在抗肿瘤方面的应用得到了广泛的关注[1].通过对DNA小沟的烷基化反应,生成或插入DNA双链最小的中间体,异喹啉可直接作用于癌细胞的DNA.异喹啉-3-甲酸及其衍生物具有抗肿瘤的潜力.我们曾报道,异喹啉-3-甲酸通过氨基酸苄酯的修饰可以提高体外抗增殖活性和体内抗肿瘤活性[2].
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