|
The pyrrolo[2,1-c][1,4]benzodiazepines (PBDs), a family of
potent DNA-binding antitumor antibiotics , are produce by
streptomyces species. These drugs react covalently with DNA to
form an N2-guanine adduct that lies within the minor groove of
DNA. Although they have the highly antitumor activity, they
produce cardiotoxicity, which have precluded their continued
clinical application. Therefore , we design and synthesis of
hybrid agents base upon the PBD and indole carboxylate (IC). The
hybrid agents were synthesized in eleven steps with 19~45%
yields. The biological activities of these drugs are under
investigation.
|