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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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-11, Vol.8 (22), p.3133-3136
Hauptverfasser:	Smith, Amos B., Sasho, Setsuya, Barwis, Bari A., Sprengeler, Paul, Barbosa, Joseph, Hirschmann, Ralph, Cooperman, Barry S.
Format:	Artikel
Sprache:	eng
Schlagworte:	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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Zusammenfassung:	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