| abstract |
Disclosed are indol-alkyl-amines as represented by the general formula (I), which are inhibitors of the interaction between MDM2 and p53, where X is C(=O) or CHR8; -QY< is -CR9=C<, -CHR9-CH< or -CHR9-N<; R9 is hydrogen or alkyl; R1 is hydrogen, aryl, heteroaryl, alkyloxycarbonyl, alkyl, or substituted-alkyl; R2 is hydrogen, halo, alkyl, alkyloxy, arylalkyloxy, heteroaryIalkyloxy, phenylthio, hydroxyalkylcarbonyl, substituted-alkyl or substituted- cycloalkyl; R3 is hydrogen, alkyl, heteroaryl, cycloalkyl, substituted-alkyl or substituted- cycloalkyl; R4 and R5 are each independently hydrogen, halo, alkyl, polyhaloalkyl, cyano, cyanoalkyl, hydroxy, amino or alkyloxy; or R4 and R5 together can optionally form a bivalent radical selected from methylenedioxy or ethylenedioxy; R6 is hydrogen, alkyloxycarbonyl or alkyl; Z is a heteroaryl moiety; and the remaining substituents are as defined herein. Also disclosed is the use of a compound as defined above for the manufacture of a medicament for treating cancer. |