| Abstract
| - The 9-aminoacridine chromophore is an important buildingblock of DNA-targeted chemotherapeutic agents. The successof 1-[2-(acridin-9-ylamino)ethyl]-1,3-dimethylthiourea as acarrier group in cytotoxic platinum−intercalator conjugatesprompted us to explore the synthesis of an analogousguanidine-functionalized acridine. In a successful effort togenerate such a derivative, various methods of guanidylationwere employed, which demonstrate that the acridine C9−N9 linkage is highly susceptible to electrophilic and nucleophilic attack. The newly established reactivities provideefficient pathways to novel cyclic and spirocyclic acridinederivatives.
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