BIOREDUCTIVELY-ACTIVATED PRODRUGS

摘要

The present invention relates to a compound of formula (1), or a pharmaceutically acceptable salt thereof, wherein: Ar is a substituted aryl or heteroaryl group bearing at least one nitro or azido group or is a group of formula (2) or (3) wherein R1, and R2, which may be the same or different ar e independently optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, aryl, COR3 or, together with the intervening carbon atom, form an optionally substituted heterocycloalkyl or carbocyclic ring ; L is -OC(O)- or -OP(O)(OR6)-; n is0or1;X is 0, S, NR7 or a single covalent bond; R3 is OR4 or NR4R5; R4, R5, R6 and R7 are each independently hydrogen or optionally substituted alkyl or, where Rr is NR4R5, R4 and R5 ca n be joined to form, together with the intervening nitrogen atom, a heterocycloalkyl ring; R8 is hydrogen, alkoxy or diatkylaminoalkyl; R9 is optionally substituted alkyl; R10 is hydrogen, alkyl, alkoxy or dialkylaminoalkyl; R11 and R12 are independently hydrogen, alkyl, alkoxy, thioatkoxy, amino, alkylamino, dialkylamino, morpholino, piperidino,piperazi no or l-aziridinyl; A is an optionally substituted aryl or heteroaryl ring; and Dr is a moiety such that DrXH represents a cytotoxic or cytostatic compound.