The pyrrolo[2,1-c][1,4]benzodiazepine (PDB) antitumor antibiotics are a well-known class of sequence-selective DNA-binding agents. 1 Among the PDB family, anthramycin (Fig. 1) have shown significant in vitro cytotoxicity but have not progressed in clinical trials due to side effects (cardiotoxicity,…). Improvements to enhance antitumor potency and to surmount this drawback have been done. 2 Nevertheless the need for analogous structures was still of interest. 3. ...