甲基呋喃核苷衍生物的设计合成与抗肿瘤活性Designand-药学学报.PDF

药学学报 Acta Pharmaceutica Sinica 2009, 44 (7) : 747753 ·747 · 3- 甲基呋喃核苷衍生物的设计合成与抗肿瘤活性 * 史丽鸿, 金东哲, 周伟澄, 王 娟, 陈秀华 (上海医 工业研究院, 创新 物与制药工艺国家重点实验室, 上海 200437) 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 1 17 个3- 甲基呋喃核苷类新化合物, 其结构经 H 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 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。 关键词: 甲基呋喃核苷; 合成; 抗肿瘤活性 中图分类号: R916.1 文献标识码:A 文章编号: 0513-4870 (2009) 07-0747-07 Design and synthesis of 3-methyl-furanonucleosides and their anti-tumor activities * SHI Li-hong , JIN Dong-zhe, ZHOU Wei-cheng, WANG Juan, CHEN Xiu-hua (State Key Laboratory of New Drug and Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, Shanghai 200437, China) 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. Key words: methylfuranonucleoside; synthesis; anti-tumour activity 恶性肿瘤是严重威胁人类健康的一种常见疾病, K562、白血病K562IU 和乳腺癌MCF-7 等较 1- 甲基 尽管迄今尚未发现根治肿瘤的药物,