Abstract: Several acridine derivatives were synthesized and their anti-proliferative activity was determined. The most active molecules were derivatives of 5-methylacridine-4-carboxylic acid. The DNA binding properties of the synthesized acridines were analyzed by competitive dialysis and compared with the anti-proliferative activities. While inactive acridine derivatives showed high selectivity for G-quadruplex structures, the most active 5-methylacridine-4-carboxamide derivatives had high affinity for DNA but showed poor specificity. An NMR titration study was performed with the most active 5-methylacridine-4-carboxamide, confirming the high affinity of this compound for both duplex and quadruplex DNAs.
This is an open access article distributed under the
Creative Commons Attribution License which permits unrestricted use, distribution,
and reproduction in any medium, provided the original work is properly cited.
Export to BibTeX
MDPI and ACS Style
Ferreira, R.; Aviñó, A.; Mazzini, S.; Eritja, R. Synthesis, DNA-Binding and Antiproliferative Properties of Acridine and 5-Methylacridine Derivatives. Molecules 2012, 17, 7067-7082.
Ferreira R, Aviñó A, Mazzini S, Eritja R. Synthesis, DNA-Binding and Antiproliferative Properties of Acridine and 5-Methylacridine Derivatives. Molecules. 2012; 17(6):7067-7082.
Ferreira, Rubén; Aviñó, Anna; Mazzini, Stefania; Eritja, Ramon. 2012. "Synthesis, DNA-Binding and Antiproliferative Properties of Acridine and 5-Methylacridine Derivatives." Molecules 17, no. 6: 7067-7082.