Selective inhibition of c-Myc/max dimerization by a pyrazolo[1,5-a]- pyrimidine

Abstract

(Chemical Equation Presented) 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. © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.