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Preparation of 5 '-deoxy-5 '-amino-5 '-C-methyl adenosine derivatives and their activity against DOT1L

文献类型：期刊论文

作者Liu, Tongchao2,3; Xie, Wuchen1,3; Li, Cong4,5; Ren, Huanming1,3; Mao, Yudong3; Chen, Guohua1; Cheng, Maosheng2; Zhao, Dongmei2; Shen, Jingkang3,5; Li, Jia4,5
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2017-11-15
卷号27期号:22页码:4960-4963
关键词5'-Deoxy-5'-amino-5'-C-methyl adenosine derivative N-glycosylation Nucleoside synthesis DOT1L inhibitor Structure activity relationship
ISSN号0960-894X
DOI10.1016/j.bmcl.2017.10.019
文献子类Article
英文摘要From a readily available 5-C-Me ribofuranoside, we have realized a reliable route to valuable 5'-deoxy-5'-amino-5'-C-methyl adenosine derivatives at gram scale with confirmed stereochemistry. These adenosine derivatives are useful starting materials for the preparation of 5'-deoxy-5'-amino-5'-C-methyl adenosine derivatives with higher complexity. From one of the new adenosine derivatives, some 5'-deoxy-5'-amino-5'-C-methyl adenosine DOT1L inhibitors were prepared in several steps. Data from DOT1L assay indicated that additional 5'-C-Me group improved the enzyme inhibitory activity. (C) 2017 Elsevier Ltd. All rights reserved.
WOS关键词HISTONE METHYLTRANSFERASE DOT1L ; MYCOBACTERIUM-TUBERCULOSIS ; SIDEROPHORE BIOSYNTHESIS ; MEDICINAL CHEMISTRY ; INHIBITORS ; POTENT ; ANALOGS ; LEUKEMIA ; EPZ-5676 ; TARGET
资助项目National Natural Science Foundation of China[81673309] ; National Science AMP[00000000] ; Technology Major Project "Key New Drug Creation and Manufacturing Program", China[2014ZX09507-002] ; Chinese Academy of Sciences[XDA12020310] ; program for Innovative Research Team of the Ministry of Education[00000000] ; program for Liaoning Innovative Research Team at Shenyang Pharmaceutical University[00000000]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000414000000004
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/272403]  
专题国家新药筛选中心
中科院受体结构与功能重点实验室
新药研究国家重点实验室
药物化学研究室
通讯作者Zhao, Dongmei; Zhou, Yubo; Xiong, Bing; Chen, Yue-Lei
作者单位1.China Pharmaceut Univ, Sch Pharm, 24 Tongjiaxiang, Nanjing 210009, Jiangsu, Peoples R China;
2.Shenyang Pharmaceut Univ, Minist Educ, Key Lab Struct Based Drug Design & Discovery, Shenyang 110016, Liaoning, Peoples R China;
3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China;
4.Natl Ctr Drug Screening, 189 Guoshoujing Rd, Shanghai 201203, Peoples R China;
5.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714		 Liu, Tongchao,Xie, Wuchen,Li, Cong,et al. Preparation of 5 '-deoxy-5 '-amino-5 '-C-methyl adenosine derivatives and their activity against DOT1L[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2017,27(22):4960-4963.
APA Liu, Tongchao.,Xie, Wuchen.,Li, Cong.,Ren, Huanming.,Mao, Yudong.,...&Chen, Yue-Lei.(2017).Preparation of 5 '-deoxy-5 '-amino-5 '-C-methyl adenosine derivatives and their activity against DOT1L.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,27(22),4960-4963.
MLA Liu, Tongchao,et al."Preparation of 5 '-deoxy-5 '-amino-5 '-C-methyl adenosine derivatives and their activity against DOT1L".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 27.22(2017):4960-4963.

入库方式： OAI收割

来源：上海药物研究所

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