Selective metal cation activation of a DNA alkylating agent: synthesis and evaluation of methyl 1,2,9,9a-tetrahydrocyclopropa[c]pyrido[3,2-e]indol-4-one-7-carboxylate (CPyI)

Results show that CPyI analogues possess identical DNA alkylation sequence selectivity and DNA alkylation efficiencies and are activted by metal cations. Data further suggest that even with structural changes in the alkylation subunit, CPyI analogues retain their potent cytotoxic activity.