We designed and synthesized the hybrid 6, prepared combining the minor groo
ve binders distamycin A and pyrrolo [2,1-c][1,4] benzodiazepine (PBD) 4, re
lated to the natural occurring anthramycin (2) and DC-81 (3). In this paper
, the effects of the compound 6 on molecular interactions between DNA and t
ranscription factor Spl were studied. The results obtained demonstrate that
PBD-distamycin hybrid is a powerful inhibitor of Sp1/DNA interactions.