Convenient preparation of pinometostat and related 5 '-deoxy-5 '-amino adenosine derivatives as well as their activity against DOT1L

doi:10.1016/j.tetlet.2017.12.064

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	Convenient preparation of pinometostat and related 5 '-deoxy-5 '-amino adenosine derivatives as well as their activity against DOT1L
	Liu, Tongchao 1,2; Ren, Huanming 2,4; Li, Cong 3; Chen, Guohua 4; Cheng, Maosheng 1; Zhao, Dongmei 1; Shen, Jingkang 2,5; Li, Jia3,5 ; Zhou, Yubo3,5 ; Xiong, Bing2,5
刊名	TETRAHEDRON LETTERS
	2018-01-24
卷号	59 期号:4 页码:415-417
关键词	DOTI L inhibitor Pinometostat Amination 5 '-Deoxy-5 '-amino adenosine derivative Structure activity relationship
ISSN号	0040-4039
DOI	10.1016/j.tetlet.2017.12.064
文献子类	Article
英文摘要	From adenosine and 2'-C-Me adenosine, a 3-step route towards nucleoside DOT1L inhibitors, including pinometostat, EPZ5677, and FED1, was established. With useful structural-activity relationship information, the newly prepared 2'-C-Me adenosine derivatives contribute to the limited repertoire of ribose modified nucleoside DOT1L inhibitors. In general, this new synthetic method will facilitate not only the study of nucleoside DOT1L inhibitors, but also the synthetic and medicinal chemistry research of 5'-deoxy-5'-amino adenosine derivatives. (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] ; "Personalized Medicines - Molecular Signature-based Drug Discovery and Development", Strategic Priority Research Program of the 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 ; POTENT ; INHIBITORS ; LEUKEMIA
WOS研究方向	Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000424067200021
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/279949]
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.Shenyang Pharmaceut Univ, Key Lab Struct Based Drug Design & Discovery, Minist Educ, 103 Wenhua Lu, Shenyang 110016, Liaoning, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; 3.Natl Ctr Drug Screening, 189 Guoshoujing Rd, Shanghai 201203, Peoples R China; 4.China Pharmaceut Univ, Sch Pharm, 24 Tongjiaxiang, Nanjing 210009, Jiangsu, 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,Ren, Huanming,Li, Cong,et al. Convenient preparation of pinometostat and related 5 '-deoxy-5 '-amino adenosine derivatives as well as their activity against DOT1L[J]. TETRAHEDRON LETTERS,2018,59(4):415-417.
APA	Liu, Tongchao.,Ren, Huanming.,Li, Cong.,Chen, Guohua.,Cheng, Maosheng.,...&Chen, Yue-Lei.(2018).Convenient preparation of pinometostat and related 5 '-deoxy-5 '-amino adenosine derivatives as well as their activity against DOT1L.TETRAHEDRON LETTERS,59(4),415-417.
MLA	Liu, Tongchao,et al."Convenient preparation of pinometostat and related 5 '-deoxy-5 '-amino adenosine derivatives as well as their activity against DOT1L".TETRAHEDRON LETTERS 59.4(2018):415-417.