Conformationally constrained nucleoside phosphonic acids--potent inhibitors of human mitochondrial and cytosolic 5'(3')-nucleotidases

This work describes novel in vitro inhibitors of human mitochondrial (mdN) and cytosolic (cdN) 5'(3')-deoxynucleotidases. We designed a series of derivatives of the lead compound (S)-1-[2-deoxy-3,5-O-(phosphonobenzylidene)-β-d-threo-pentofuranosyl]thymine bearing various substituents in th...

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Published in:	Organic & biomolecular chemistry 2014-10, Vol.12 (40), p.7971-7982
Main Authors:	Šimák, Ondřej, Pachl, Petr, Fábry, Milan, Buděšínský, Miloš, Jandušík, Tomáš, Hnízda, Aleš, Skleničková, Radka, Petrová, Magdalena, Veverka, Václav, Řezáčová, Pavlína, Brynda, Jiří, Rosenberg, Ivan
Format:	Article
Language:	English
Subjects:	5'-Nucleotidase - antagonists & inhibitors 5'-Nucleotidase - metabolism Cytosol - enzymology Dose-Response Relationship, Drug Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Humans Mitochondria - enzymology Molecular Conformation Organophosphonates - chemical synthesis Organophosphonates - chemistry Organophosphonates - pharmacology Structure-Activity Relationship
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