Synthesis and biological evaluation of novel all-hydrocarbon cross-linked aza-stapled peptides?
Organic & Biomolecular Chemistry Pub Date: 2022-09-28 DOI: 10.1039/D2OB01496C
Abstract
Novel all-hydrocarbon cross-linked aza-stapled peptides were designed and synthesized for the first time by ring-closing metathesis between two aza-alkenylglycine residues. Three aza-stapled peptidic analogues based on the peptide dual inhibitor of p53-MDM2/MDMX interactions were synthesized and screened for biological activities. Among the three aza-stapled peptides, aSPDI-411 displayed increased anti-tumor activity, binding affinities to both MDM2 and MDMX, and cell membrane permeability compared to its linear peptide counterpart.
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Journal Name：Organic & Biomolecular Chemistry
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CAS no.: 89640-58-4
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