A review with 67 refs. DNA minor-groove binding drugs have been extensively studied in the last years to influence the regulation of gene expression in neoplastic disorders by specific interactions with DNA bases. Pyrrolo[2,1-c][1,4]benzodiazepines (PBDs), CC-1065 and distamycins are three classes of minor-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, to either modify the reactivity profile or introduce extra interactions within the minor groove, thus changing the binding site or modulating the binding sequence.
DNA minor-groove binders: results and design of new antitumor agents
BARALDI, Pier Giovanni;CACCIARI, Barbara;ROMAGNOLI, Romeo;
1999
Abstract
A review with 67 refs. DNA minor-groove binding drugs have been extensively studied in the last years to influence the regulation of gene expression in neoplastic disorders by specific interactions with DNA bases. Pyrrolo[2,1-c][1,4]benzodiazepines (PBDs), CC-1065 and distamycins are three classes of minor-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, to either modify the reactivity profile or introduce extra interactions within the minor groove, thus changing the binding site or modulating the binding sequence.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
