Design, synthesis and cellular metabolism study of 4'-selenonucleosides.

Abstract:

BACKGROUND:4'-seleno-homonucleosides were synthesized as next-generation nucleosides, and their cellular phosphorylation was studied to confirm the hypothesis that bulky selenium atom can sterically hinder the approach of cellular nucleoside kinase to the 5'-OH for phosphorylation. RESULTS:4'-seleno-homonucleosides (n = 2), with one-carbon homologation, were synthesized through a tandem seleno-Michael addition-SN2 ring cyclization. LC-MS analysis demonstrated that they were phosphorylated by cellular nucleoside kinases, resulting in anticancer activity. CONCLUSION:The bulky selenium atom played a key role in deciding the phosphorylation by cellular nucleoside kinases. [Formula: see text].

journal_name

Future Med Chem

authors

Yu J,Sahu PK,Kim G,Qu S,Choi Y,Song J,Lee SK,Noh M,Park S,Jeong LS

doi

10.4155/fmc.15.102

subject

Has Abstract

pub_date

2015-01-01 00:00:00

pages

1643-55

issue

13

eissn

1756-8919

issn

1756-8927

journal_volume

7

pub_type

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