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1. Synthesis and biological evaluation of 1,1-difluoro-2-(tetrahydro-3-furanyl)ethylphosphonic acids possessing a N9-purinylmethyl functional group at the ring. a new class of inhibitors for purine nucleoside phosphorylases.

Author

Yokomatsu T, Hayakawa Y, Suemune K, Kihara T, Soeda S, Shimeno H, and Shibuya S

Subjects
Antineoplastic Agents chemical synthesis, Antineoplastic Agents pharmacology, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors pharmacology, Erythrocytes enzymology, Fluorine Compounds pharmacology, Furans pharmacology, Gram-Positive Asporogenous Rods enzymology, Humans, Inosine metabolism, Molecular Structure, Organophosphonates pharmacology, Phosphorylation, Purines pharmacology, Fluorine Compounds chemical synthesis, Furans chemical synthesis, Organophosphonates chemical synthesis, Purine-Nucleoside Phosphorylase antagonists & inhibitors, Purines chemical synthesis
Abstract

1,1-Difluoro-2-(tetrahydro-3-furanyl)ethylphosphonic acids cis-3 and trans-3 possessing a N9-purinylmethyl functionality at the ring were synthesized and tested as "multi-substrate analogue" inhibitors for purine nucleoside phosphorylases. Radical cyclization of allyic alpha,alpha-difluorophosphonate (E)-7 was applied to construct the alpha,alpha-difluorophosphonate-functionalized tetrahydrofuranyl moiety. The IC50 values of cis-3 and trans-3 for human erythrocyte PNP-catalyzed phosphorylation of inosine were determined to be 88 and 320 nM, respectively. The stereochemistry of the inhibitors was found to affect significantly the inhibitory potency.

Published
1999
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