Document Detail


N-PHOSPHONOCARBONYLPYRROLIDINE DERIVATIVES OF GUANINE: A NEW CLASS OF BI-SUBSTRATE INHIBITORS OF HUMAN PURINE NUCLEOSIDE PHOSPHORYLASE.
MedLine Citation:
PMID:  22264015     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
A complete series of pyrrolidine nucleotides, (3R)- and (3S)-3-(guanin-9-yl)pyrrolidin-1-N-ylcarbonylphosphonic acids and (3S,4R)-, (3R,4S)-, (3S,4S)-, and (3R,4R)-4-(guanin-9-yl)-3-hydroxypyrrolidin-1-N-ylcarbonylphosphonic acids, were synthesised and evaluated as potential inhibitors of purine nucleoside phosphorylase (PNP) isolated from peripheral blood mononuclear cells (PBMCs) and cell lines of myeloid and lymphoid origin. Two compounds, 2a (S)-3-(guanin-9-yl)pyrrolidin-1-N-ylcarbonylphosphonic acid and 6a (3S,4R)-4-(guanin-9-yl)-3-hydroxypyrrolidin-1-N-ylcarbonylphosphonic acid were recognised as nanomolar competitive inhibitors of PNP isolated from cell lines with Ki values within the ranges of 16-100 nM and 10-24 nM, respectively. The low MESGKi and PiKi values of both compounds for PNP isolated from PBMCs suggest that these compounds could be bi-substrate inhibitors that occupy both the phosphate and nucleoside binding sites of the enzyme.
Authors:
Dominik Rejman; Natalya Panova; Pavel Klener; Bokang Maswabi; Radek Pohl; Ivan Rosenberg
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-1-23
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  -     ISSN:  1520-4804     ISO Abbreviation:  -     Publication Date:  2012 Jan 
Date Detail:
Created Date:  2012-1-23     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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