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

doi:10.1016/j.bmcl.2017.10.019

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	Preparation of 5 '-deoxy-5 '-amino-5 '-C-methyl adenosine derivatives and their activity against DOT1L
	Liu, Tongchao 2,3; Xie, Wuchen 1,3; Li, Cong 4,5; Ren, Huanming 1,3; Mao, Yudong 3; Chen, Guohua 1; Cheng, Maosheng 2; Zhao, Dongmei 2; Shen, Jingkang 3,5; Li, Jia4,5
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	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
DOI	10.1016/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.
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关键词	HISTONE METHYLTRANSFERASE DOT1L ; MYCOBACTERIUM-TUBERCULOSIS ; SIDEROPHORE BIOSYNTHESIS ; MEDICINAL CHEMISTRY ; INHIBITORS ; POTENT ; ANALOGS ; LEUKEMIA ; EPZ-5676 ; TARGET
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000414000000004
内容类型	期刊论文
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.