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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.
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