Diamidine compounds useful as DNA minor groove binders

摘要

A diamidine derivative has the formula (I) wherein: X is O, S, or NH; Y is CH or N; A is CH or N; B is NH, O or S; R1 is H, alkyl, halogen, oxyalkyl, oxyaryl or oxyarylalkyl; R2 and R9 are each independently H, hydroxy, alkyl, cycloalkyl, aryl, alkylaryl, alkoxyalkyl, hydroxycycloalkyl, alkoxycycloalkoxy, hydroxyalkyl, aminoalkyl or alkylaminoalkyl; R3, R4, R13 and R14 are each independently H, alkyl, alkoxyalkyl, cycloalkyl, aryl, alkylaryl, hydroxyalkyl, aminoalkyl, or alkylaminoalkyl, or R3 and R4 together or R13 and R14 together represent alkyl, hydroxyalkyl, or alkylene, or R3 and R4 together or R13 and R14 together are an optionally substituted 1,2-phenylene L is a group of formula (2) and R5, R6, R7, and R8 are each of H, alkyl, halo, aryl, arylalkyl, aminoalkyl, aminoaryl, oxoalkyl, oxoaryl or oxoarylalkyl. The compounds of formula I bind the minor groove of DNA as a dimer.