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

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Liu T,Xie W,Li C,Ren H,Mao Y,Chen G,Cheng M,Zhao D,Shen J,Li J,Zhou Y,Xiong B,Chen YL

doi

10.1016/j.bmcl.2017.10.019

subject

Has Abstract

pub_date

2017-11-15 00:00:00

pages

4960-4963

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(17)30994-0

journal_volume

27

pub_type

杂志文章

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