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中文摘要：
抑制DNA的合成是阻断癌细胞扩散的主要策略，核苷类化合物能有效地掺入DNA并且终止DNA链的延伸。到目前为止，有20多个核苷化合物为抗癌药物。本项目计划设计合成一系列4'-叠氮-2'-脱氧-2'-氟胞嘧啶核苷类似物，测试其生物活性，特别是抗肿瘤的活性；研究该类核苷化合物的结构与活性关系。并深入探讨其作用机制，期望从中筛选出具有良好抗肿瘤活性，同时毒性较小的抗肿瘤新药先导化合物。为该类化合物的进一步研究与开发奠定基础。
英文摘要：
nucleoside analogs；synthesis；antitumor activity；structure-activity relationship；
结论摘要：
按期完成了各项研究任务，筛选出了具有良好抗肿瘤活性的先导化合物。本课题设计并合成四类共60个新型的4'-叠氮-2'-脱氧-2'-氟胞嘧啶核苷类似物；通过在不同的肿瘤细胞株上进行活性筛选、构效关系研究，目前已经遴选出一个具有良好抗肝癌活性的先导化合物；并对其在小鼠体内进行了急性毒性与药效学等试验研究，更为深入的临床前研究实验研究工作目前正在进行当中。此外，对该化合物的药物作用机制也进行了探讨和初步的研究。在该项目的资助下在J. Med. Chem., Antivir. Ther., Antivir. Res., Eur. J. Med. Chem., Asian Pac. J. Cancer P.等期刊上发表研究论文30余篇，申请发明专利2项（已授权，其中PCT 1项），培养博士研究生3名，硕士研究生8名。
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期刊论文
A New Route for the Synthesis of 4-Amino-5-Fluoro-7-(2-Deoxy-2-Fluoro-2-C-Methyl--d- Ribofuranosyl)-
Synthesis of novel strobilurin-pyrimidine derivatives and their antiproliferative activity against h
Investigation of the interaction between five alkaloids and human hemoglobin by fluorescence spectro
Palladium-Catalysed Synthesis of 9H-Pyrrolo[1,2-a]indol-9-ones and the Isomeric Indeno[2,1-b]pyrrol-
I2-Mediated Oxidative C-O Bond Formation for the Synthesis of 1,3,4-Oxadiazoles from Aldehydes and H
Azvudine, A Novel Nucleoside Reverse Transcriptase Inhibitor Showed Good Drug Combination Features a
I-Mediated Oxidative C-N Bond Formation for Metal-Free One-Pot Synthesis of Di-, Tri-, and Tetrasubs
A concise approach to polysubstituted oxazoles from N-acyl-2-bromo enamides via a copper(I)/amino ac
Enantiopure azetidine-2-carboxamides as organocatalysts for direct asymmetric aldol reactions in aqu
Lewis acid-catalyzed tandem acylation-Nazarov cyclization for the syntheses of fused cyclopentenones
Investigation of the interaction between isomeric derivatives and human serum albumin by fluorescenc
Synthesis and Biological Evaluation of 4-Substituted Fluoronucleoside Analogs for the Treatment of H
Synthesis of 2-Amino-1,3,4-oxadiazoles and 2-Amino-1,3,4-thiadiazoles via Sequential Condensation an
Investigation of the Binding Between Pepsin and Nucleoside Analogs by Spectroscopy and Molecular Sim
Anti-hepatitis B Virus Activity of alpha-DDB-FNCG, a Novel Nucleoside-Biphenyldicarboxylate Compound
Study of the interaction between bovine hemoglobin and analogs of biphenyldicarboxylate by spectrofl
Lewis acid-catalyzed tandem acylation―Nazarov cyclization for the syntheses of fused cyclopentenones
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