DNA minor-groove binders: results and design of new antitumor agents

Farmaco. 1999 Jan-Feb;54(1-2):15-25. doi: 10.1016/s0014-827x(98)00102-5.

Abstract

DNA minor-groove binding drugs have been extensively studied in the last years in order to influence the regulation of gene expression in neoplastic disorders by means of 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, in order to either modify the reactivity profile or introduce extra interactions within the minor groove, thus changing the binding site or modulating the binding sequence.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / metabolism*
  • Antineoplastic Agents / pharmacology*
  • Binding Sites
  • DNA, Neoplasm / drug effects*
  • DNA, Neoplasm / metabolism*
  • Humans

Substances

  • Antineoplastic Agents
  • DNA, Neoplasm