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Selective Inhibition of c‐Myc/Max Dimerization by a Pyrazolo[1,5‐ a ]pyrimidine
Author(s) -
Kiessling Anke,
Wiesinger Rita,
Sperl Bianca,
Berg Thorsten
Publication year - 2007
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200600294
Subject(s) - pyrimidine , chemistry , stereochemistry , pharmacology , biology
c‐Myc/Max Dimerization. The interaction between the oncoprotein c‐Myc and its activation partner Max is considered to be a desirable target for cancer drug development. However, the interaction is mediated by large α‐helical interfaces without obvious binding sites for small molecule inhibitors. This paper describes the identification of a substitution pattern for pyrazolopyrimidines which appears to be associated with activity against this challenging target.