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Updated: May 1, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Designer macrocyclic organo-peptide hybrids inhibit the interaction between p53 and HDM2/X by accommodating a
Jessica M Smith1, John R Frost, Rudi Fasan
1Department of Chemistry, University of Rochester, Rochester, NY, USA. fasan@chem.rochester.edu.
Abstract:
We report the design of side-chain-to-tail linked organo-peptide hybrids incorporating an α-helical protein-binding motif. Using this strategy, macrocyclic inhibitors of the p53:HDM2 interaction displaying dual specificity against the HDMX homolog as well as increased proteolytic stability could be obtained.
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