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.
Synthesis, DNA-Binding and Antiproliferative Properties of Acridine and 5-Methylacridine Derivatives / R. Ferreira, A. Avinò, S. Mazzini, R. Eritja. - In: MOLECULES. - ISSN 1420-3049. - 17:6(2012), pp. 7067-7082.
|Titolo:||Synthesis, DNA-Binding and Antiproliferative Properties of Acridine and 5-Methylacridine Derivatives|
MAZZINI, STEFANIA (Penultimo)
|Parole Chiave:||Acridine; DNA-binding drugs; G-quadruplex; NMR; Solid-phase synthesis|
|Settore Scientifico Disciplinare:||Settore CHIM/06 - Chimica Organica|
|Data di pubblicazione:||2012|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.3390/molecules17067067|
|Appare nelle tipologie:||01 - Articolo su periodico|