Bioreductively activated stilbene prodrugs

Abstract

A compound of formula (1), or a pharmaceutically acceptable salt thereof, wherein Ar is a substituted heteroaryl group bearing at least one nitro or azido group or is a group of formula (2) or (3); R1 is hydrogen, optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl; R2 is alkyl, alkoxy, thialkoxy or halo; R3, R4 and R5 are each independently alkyl, alkoxy, thialkoxy or halo with the proviso that at least two of R3, R4 or R5 are alkoxy; L is —OC(O)— or —OP(O)(OR6)—; n is 0 or 1; X is O, S or NR7; Y is hydrogen, alkyl, alkoxy, thialkoxy, halo, hydroxy or dihydrogenphosphate; R6 is hydrogen or alkyl; R7 is hydrogen or alkyl; R8 is hydrogen, alkoxy or dialkylaminoalkyl; R9 is optionally substituted alkyl; R10 is hydrogen, alkyl, alkoxy or dialkylaminoalkyl; R11, and R12 are independently hydrogen, alkyl, alkoxy, thialkoxy, amono alkylamino, dialkylamino, morpholino, alkylmorpholino, piperidino, alkylpiperidiono, piperazino, alkylpiperazino or 1-aziridinyl; and A, together with the carbon atoms to which it is fused, is an optionally substituted aryl or heteroaryl ring.

Dependencies are inferred from the claim text.