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Aromatic Oligoamide Foldamers with a “Wet Edge” as Inhibitors of the α‐Helix‐Mediated p53– h DM2 Protein–Protein Interaction
Author(s) -
Prabhakaran Panchami,
Barnard Anna,
Murphy Natasha S.,
Kilner Colin A.,
Edwards Thomas A.,
Wilson Andrew J.
Publication year - 2013
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.201300069
Subject(s) - chemistry , substituent , monomer , oligomer , alkyl , alkylation , solubility , helix (gastropod) , stereochemistry , combinatorial chemistry , organic chemistry , polymer , ecology , snail , biology , catalysis
This paper describes the design, synthesis and structural analysis of a 3‐ O ‐alkylated aromatic oligoamide that incorporates an additional hydrophilic 6‐ O ‐alkyl substituent in the central monomer. This oligomer exhibits low μ M inhibitory potency against the p53– h DM2 interaction compared with its unfunctionalised counterpart and significantly improved solubility.