3'-甲基呋喃核苷衍生物的设计合成与抗肿瘤活性

Design and synthesis of 3'-methyl-furanonucleosides and their anti-tumor activities

摘要:
以具有良好抗肿瘤活性的3'-甲基腺苷和克拉屈滨为先导物, 根据生物电子等排原理, 设计并合成了17个3'-甲基呋喃核苷类新化合物, 其结构经¹H NMR和MS确证。用MTT方法评价了其体外抗肿瘤活性。结果表明, 目标化合物对人肺癌细胞A549、人结肠癌细胞LOVO和人白血病细胞CEM均有不同程度的细胞毒性, 具有进一步研究的价值。

Abstract:
Taking 3'-Me-Ado (3'-methyladenosine) and Cladribine as the leading compounds, seventeen 3'-C-methyl-furanonucleosides were designed and synthesized. All the structures were confirmed by ¹H NMR and MS. The target compounds were tested in vitro against human pulmonary carcinoma A549, human colon carcinoma LOVO and human leukemia CEM by MTT assay. The results showed that these compounds possessed moderate cytotoxities.