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- Title
New Boron Containing Acridines: Synthesis and Preliminary Biological Study.
- Authors
Druzina, Anna A.; Dudarova, Nadezhda V.; Ananyev, Ivan V.; Antonets, Anastasia A.; Kaluzhny, Dmitry N.; Nazarov, Alexey A.; Sivaev, Igor B.; Bregadze, Vladimir I.
- Abstract
The synthesis of the first conjugates of acridine with cobalt bis(dicarbollide) are reported. A novel 9-azido derivative of acridine was prepared through the reaction of 9-methoxyacridine with N3CH2CH2NH2, and its solid-state molecular structure was determined via single-crystal X-ray diffraction. The azidoacridine was used in a copper (I)-catalyzed azide-alkyne cycloaddition reaction with cobalt bis(dicarbollide)-based terminal alkynes to give the target 1,2,3-triazoles. DNA interaction studies via absorbance spectroscopy showed the weak binding of the obtained conjugates with DNA. The antiproliferative activity (IC50) of the boronated conjugates against a series of human cell lines was evaluated through an MTT assay. The results suggested that acridine derivatives of cobalt bis(dicarbollide) might serve as a novel scaffold for the future development of new agents for boron neutron capture therapy (BNCT).
- Subjects
ACRIDINE derivatives; BIOSYNTHESIS; ACRIDINES; BORON-neutron capture therapy; COPPER; MOLECULAR structure
- Publication
Molecules, 2023, Vol 28, Issue 18, p6636
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules28186636