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Nucleoside and non-nucleoside IMP dehydrogenase inhibitors as antitumor and antiviral agents.
It was hypothesized that the inhibitory activity of tiazofurin is due to an attractive electrostatic interaction between the heterocyclic sulphur atom and the furanose oxygen 1 which constrain rotation about the C-glycosidic bond in tiaz ofurin and in its active anabolite TAD. Expand
2-Chloro-N6-cyclopentyladenosine: a highly selective agonist at A1 adenosine receptors
CCPA is an agonist at A1 adenosine receptors with a 4-foldHigher selectivity and 2-fold higher affinity than CPA, and a considerably higher selectivity than the standard A1 receptor agonist R-N6-phenylisopropyladenosine (R-PIA). Expand
Tiazofurine ICN Pharmaceuticals.
  • M. Grifantini
  • Medicine
  • Current opinion in investigational drugs
  • 1 October 2000
Tiazofurine is a nucleoside analog with oncolytic activity being developed by Ribapharm as a potential treatment for leukemia and is metabolized to TAD (thiazole-4-carboxamide adenine dinucleotide), an inhibitor of IMP dehydrogenase. Expand
Ribose-modified nucleosides as ligands for adenosine receptors: synthesis, conformational analysis, and biological evaluation of 1'-C-methyl adenosine analogues.
Conformational analysis based on vicinal protonminus signproton J-coupling constants and molecular mechanics calculations using the MM2 force field proved that the methyl group on C1' in adenosine has a pronounced impact on the furanose conformation by driving its conformational equilibrium toward the north, gamma+, syn form. Expand
2-Chloro-N6-[3H]cyclopentyladenosine ([3HCCPA) —a high affinity agonist radioligand for A1 adenosine receptors
Based on the subnanomolar affinity and the high selectivity for A1 receptors [3H]CCPA proved to be a useful agonist radioligand for characterization of A1 adenosine receptors also in tissues with very low receptor density. Expand
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.
2-chloro-2'-C-methyl-N6-cyclopentyladenosine (2'-Me-CCPA), which displayed a Ki value of 1.8 nM at A1 receptors, was selective for A1 vs A2A and A3 receptors by 2166- and 2777-fold, respectively, resulting in one of the most potent and A1-selective agonists so far known. Expand
2-Chloro-N 6 -( 3 H)cyclopentyladenosine (( 3 H)CCPA) - a high affinity agonist radio Iigand for A 1 adenosine receptors
Summary. The tritiated analogue of 2-chloro-N 6 -cyclo­ pentyladenosine (CCPA), an adenosine derivative with sub­ nanomolar affinity and a 10000-fold selectivity for A 1 adenosine receptors, has beenExpand
Decomposition pathways and in vitro HIV inhibitory effects of isoddA pronucleotides: toward a rational approach for intracellular delivery of nucleoside 5'-monophosphates.
The results highlight that both types of compounds act as pronucleotides, i.e. they exert their antiviral effect via intracellular delivery of the 5'-mononucleotide of isoddA. Expand