DNA alkylation sites of nitrogen mustards conjugated to polyamines and their implications for polyamine–DNA interactions

Abstract

Polyamines conjugated to the nitrogen mustard chlorambucil increase the efficiency of DNA alkylation at N⁷ of guanine by factors in the range 10³ to 10⁴; the sequence selectivity of this alkylation (the alkylation ‘finger-print’) is largely unchanged, which is consistent with flexible, electrostatic binding and incompatible with tight, sequence-specific binding of the polyamine moiety.