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 potent than 1.
Smith
A B
AB
Department of Chemistry, University of Pennsylvania, Philadelphia 19104, USA.
Sasho
S
S
Barwis
B A
BA
Sprengeler
P
P
Barbosa
J
J
Hirschmann
R
R
Cooperman
B S
BS
D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D008958:Models, Molecular; D011714:Pyrans / Q000138:chemical synthesis* / Q000494:pharmacology; D012264:Ribonucleotide Reductases / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D011714:Pyrans; D012264:Ribonucleotide Reductases