Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters
5 years ago

Preparation of 5’-Deoxy-5’-amino-5’-C-methyl adenosine Derivatives and Their Activity against DOT1L

Preparation of 5’-Deoxy-5’-amino-5’-C-methyl adenosine Derivatives and Their Activity against DOT1L
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 preparaed in several steps. Data from DOT1L assay indicated that additional 5’-C-Me group improved the enzyme inhibitory activity.

Publisher URL: www.sciencedirect.com/science

DOI: S0960894X17309940

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