中文关键词:DNA-PK抑制剂 DNA修复 抗肿瘤 合成方法 英文关键词:DNA-PKinhibitor, DNArepair, antitumor, syntheticprocess 基金项目:黑龙江省人社厅留学回国人员择优资助项目，牡丹江师范学院科研项目（MNUB201405）

作者	单位	E-mail
景云荣	牡丹江师范学院	swxjyr@126.com
魏继承	牡丹江师范学院

摘要点击次数:1009 全文下载次数:0 中文摘要: DNA依赖的蛋白激酶（DNA-PK）是肿瘤治疗的一个潜在靶点，其抑制剂具有增强放化疗敏感性的作用。STL127705是一种有效的DNA-PK抑制剂，本文采用逆合成分析，以2-甲硫醚-4-氯嘧啶-5-基甲酸乙酯为起始原料，先后经过氨化、水解、酰胺缩合、合环、氧化、取代等6步反应制备得到目标化合物，总收率为36.8%，纯度达到95.5%，产物结构通过1H-NMR、13C-NMR、MS等表征。 英文摘要: DNA-dependent protein kinase (DNA-PK) is a potential target for tumor therapy. DNA-PK inhibitor can enhance the sensitivities of tumor cells against chemotherapy and radiotherapy. STL127705 is an effective inhibitor of DNA-PK. It was prepared by retrosynthetic analysis, using 4-chloro-2-methylsulfanyl-pyrimidine-5-carboxylic acid ethyl ester as the starting material, followed by 6 steps reaction including ammonification, hydrolysis, amide condensation, cyclization, oxidation and substitution, with an overall yield of 36.8%, the purity reached 95.5% and the structure of the target compound was confirmed by 1H-NMR, 13C-NMR and MS. 查看全文查看/发表评论下载PDF阅读器 相关附件：化合物谱图版权转让声明书原始H-NMR数据 -->