Beilstein J. Org. Chem.2016,12, 1476–1486, doi:10.3762/bjoc.12.144
: cancer; cN-IIinhibitors; nucleotide; phosphonate; triazole; Introduction
Nucleotidases are an important family of enzymes involved in the metabolism of nucleotides [1]. In particular, human cytosolic 5’-nucleotidase II (cN-II) catalyses the dephosphorylation of purine 5’-monophosphate derivatives to
effectiveness of cN-IIinhibitors in the treatment of these diseases [4][5]. As a result of our interest in this area, we and others [6] have investigated a number of structure–activity relationships (SAR) [7][8] and various medicinal chemistry approaches [9][10] to identify potential cN-IIinhibitors. As part
library of seventeen 1’-triazolyl beta-hydroxyphosphonate ribonucleoside analogues was synthesized using convenient Cu(I)-catalysed cycloaddition. These derivatives were evaluated as potential cN-IIinhibitors on the purified enzyme. Two derivatives including either an aminophenyl or an amido-substituent
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Graphical Abstract
Figure 1:
Previous (UA1776, UA2201 and UA2209 [7,8]) and new 1a–q phosphonate derivatives designed as potential cN...