Inhibition of the strand transfer step of HIV-1 integrase by non-natural dinucleotides.

Abstract:

:New, non-natural dinucleotide 5'-monophosphates, with a surrogate isonucleoside component of l-related stereochemistry at the 'terminal' position, have been synthesized. Structures of 2a-c were confirmed by multinuclear NMR spectra ((1)H, (13)C, (31)P, COSY), UV hypochromicity and FAB HRMS data. These compounds are totally resistant to cleavage by 3'- and 5'-exonucleases. The dinucleotides showed remarkable selectivity for inhibition of the strand transfer step of HIV-1 integrase. To the best of our knowledge, these compounds represent only the second example of selective strand transfer inhibitors of HIV integrase.

journal_name

Bioorg Med Chem Lett

authors

Chi G,Neamati N,Nair V

doi

10.1016/j.bmcl.2004.07.050

subject

Has Abstract

pub_date

2004-10-04 00:00:00

pages

4815-7

issue

19

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)00951-5

journal_volume

14

pub_type

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