Selective Inhibition of c‐Myc/Max Dimerization by a Pyrazolo[1,5‐<i>a</i>]pyrimidine

Abstract

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.