Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume 76, Issue 9, Pages 3078-3085Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jo102422x
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Funding
- European Commission (Prokinase Consortium)
- Prostate Cancer Foundation
- Goldhirsh Foundation
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Aza-peptides are peptidomimetics in which one or more of the alpha-carbons, bearing the side-chain residues, has been replaced by a nitrogen. These peptidomimetics have been shown to be promising for the generation of drug leads and for structure-activity relationship studies. Aza-scan is the systematic replacement of amino acid residues in a given peptide with their aza counterparts. We report here an aza-scan of a potent, peptide-based PKB/Akt inhibitor, PTR6154. Procedures for microwave-assisted, Fmoc/t-Bu chemistry, solid-phase aza-peptide synthesis were developed which significantly reduce standard reaction time and are suitable for automation. Novel substituted hydrazines have been prepared for the straightforward incorporation of aza-arginine and aza-proline residues. This work will enable aza-scan to become a more common and standard method for structure-activity relationship studies of peptides.
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