DNA minor-groove binding drugs have been extensively studied in the last ye
ars in order to influence the regulation of gene expression in neoplastic d
isorders by means of specific interactions with DNA bases. Pyrrolo[2,1-c][1
,4]benzodiazepines (PBDs), CC-1065 and distamycins are three classes of min
or-groove alkylating agents which showed interesting cytotoxicity profiles,
but they cannot be used in humans for various toxicity problems. For this
reason many groups applied heterocyclic substitutions extensively, in order
to either modify the reactivity profile or introduce extra interactions wi
thin the minor groove, thus changing the binding site or modulating the bin
ding sequence. (C) 1999 Elsevier Science S.A. All rights reserved.