Design and synthesis of a tetrahydropyran-based inhibitor of mammalian ribonucleotide reductase

A tetrahydropyran-based inhibitor ( 2) of mammalian ribonucleotide reductase (mRR) has been designed and synthesized based on the heptapeptide, N-AcFTLDADF ( 1), corresponding to the C-terminus of the R2 subunit of mRR. Inhibition studies revealed that 2 is indeed a competent inhibitor, albeit less...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-11, Vol.8 (22), p.3133-3136
Main Authors: Smith, Amos B., Sasho, Setsuya, Barwis, Bari A., Sprengeler, Paul, Barbosa, Joseph, Hirschmann, Ralph, Cooperman, Barry S.
Format: Article
Language:English
Subjects:
Analytical, structural and metabolic biochemistry
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antineoplastic agents
Antiviral agents
Biological and medical sciences
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - pharmacology
Enzymes and enzyme inhibitors
Fundamental and applied biological sciences. Psychology
General aspects
Medical sciences
Models, Molecular
Oxidoreductases
Pharmacology. Drug treatments
Pyrans - chemical synthesis
Pyrans - pharmacology
Ribonucleotide Reductases - antagonists & inhibitors
Structure-Activity Relationship
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Summary:A tetrahydropyran-based inhibitor ( 2) of mammalian ribonucleotide reductase (mRR) has been designed and synthesized based on the heptapeptide, N-AcFTLDADF ( 1), corresponding to the C-terminus of the R2 subunit of mRR. Inhibition studies revealed that 2 is indeed a competent inhibitor, albeit less potent than 1. A tetrahydropyran-based inhibitor ( 2) of mammalian ribonucleotide reductase (mRR) has been designed and synthesized based on the heptapeptide, N-AcFTLDADF, corresponding to the C-terminus of the R2 subunit of mRR. Inhibition studies revealed that 2 is indeed a competent inhibitor, albeit less potent than the parent peptide.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00575-7