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Title

Synthesis, DNA-binding and antiproliferative properties of acridine and 5-methylacridine derivatives

AuthorsFerreira, Rubén ; Aviñó, Anna ; Mazzini, Stefania; Eritja Casadellà, Ramón
KeywordsDNA-binding drugs
NMR
Acridine
G-quadruplex
Solid-phase synthesis
DNA
Issue DateJun-2012
PublisherMultidisciplinary Digital Publishing Institute
CitationMolecules
AbstractSeveral 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.
Publisher version (URL)http://doi.org/10.3390/molecules17067067
URIhttp://hdl.handle.net/10261/125326
DOIhttp://dx.doi.org/10.3390/molecules17067067
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