Synthesis and biological activity of cyclic peptide inhibitors of ribonucleotide reductase

Authors
Liehr, S Barbosa, J Smith, AB Cooperman, BS
Citation
S. Liehr et al., Synthesis and biological activity of cyclic peptide inhibitors of ribonucleotide reductase, ORG LETT, 1(8), 1999, pp. 1201-1204
Citations number
28
Categorie Soggetti
Organic Chemistry/Polymer Science
Journal title
ORGANIC LETTERS
ISSN journal
15237060 → ACNP
Volume
1
Issue
8
Year of publication
1999
Pages
1201 - 1204
Database
ISI
SICI code
1523-7060(19991021)1:8<1201:SABAOC>2.0.ZU;2-T
Abstract
[GRAPHICS] A series of lactam-bridged peptide inhibitors (2-6) of mammalian ribonucleo tide reductase (mRR) has been designed and synthesized on the basis of the heptapeptide N-AcFTLDADF (1), corresponding to the C-terminus of the R2 sub unit of mRR. Inhibition studies revealed a direct relation between ring siz e and activity, with peptide 5 being 2.5 times more potent than peptide 1.