| The synthesis and biological evaluation of benzamide riboside and its phosphordiamidates prodrugs | |
| Zhou, Jianning ; Tan, Chunyan ; Zhang, Nan ; Fan, Jian ; Guo, Chun ; Jiang, Yuyang | |
| 2010-05-10 ; 2010-05-10 | |
| 会议名称 | PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS ; 17th International Conference on Phosphorus Chemistry ; Xiamen, PEOPLES R CHINA ; Web of Science |
| 关键词 | benzamide riboside prodrug benzylphosphordiamidate IMP DEHYDROGENASE INHIBITOR Chemistry, Inorganic & Nuclear |
| 中文摘要 | In order to overcome the drug resistance and enhance the membrane penetration ability of benzamide riboside [BR, (1-beta-D-ribofuranosyl) benzene-3-carboxamide], which is a novel C-glycoside analogue of nicotinamide riboside and has excellent cytotoxic activity, we designed and synthesized two phosphordiamidates (1a and 1b) as prodrugs to deliver phosphorylated BR into cells. However; the bioactivity evaluation shows that la and 1b have lower biological activity (IC50 > 200 mu M and 173 p,M, respectively) compared to BR. This might be due to the fact that la and 1b could only serve as the BR depot form and thus could not be metabolized to the phosporylatd benzamide riboside. |
| 会议录出版者 | TAYLOR & FRANCIS LTD ; ABINGDON ; 4 PARK SQUARE, MILTON PARK, ABINGDON OX14 4RN, OXON, ENGLAND |
| 语种 | 英语 ; 英语 |
| 内容类型 | 会议论文 |
| 源URL | [http://hdl.handle.net/123456789/19983]  |
| 专题 | 清华大学 |
| 推荐引用方式 GB/T 7714 | Zhou, Jianning,Tan, Chunyan,Zhang, Nan,et al. The synthesis and biological evaluation of benzamide riboside and its phosphordiamidates prodrugs[C]. 见:PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, 17th International Conference on Phosphorus Chemistry, Xiamen, PEOPLES R CHINA, Web of Science. |
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