The DNA minor groove is an attractive target for the design and development of mols. able to specifically recognize predetd. DNA sequences. The pyrrole-amide skeleton of distamycin A has been also used as DNA sequence selective vehicle for the delivery of alkylating functions to DNA targets. Selectivity for specific sequences may be of particular importance in affecting the activity of regulatory genes (oncogenes and tumor suppressor genes). Recent work on a no. of hybrid compds., in which known antitumor compds. or simple active moieties of known antitumor agents have been tethered to distamycin frame or hairpin polyamides derived from distamycin, is reviewed. The DNA alkylating and growth inhibition activities against several tumor cell lines are reported and discussed in terms of their structural differences in relation to both the no. of N-Me pyrrolic rings and the type of the alkylating unit tethered to the oligopyrrolic frame
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