Synthesis, DNA-binding and antiproliferative properties of acridine and 5-methylacridine derivatives |
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Authors: | Ferreira Rubén Aviñó Anna Mazzini Stefania Eritja Ramon |
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Affiliation: | Institute for Research in Biomedicine, Baldiri Reixac 10, E-08028 Barcelona, Spain. ruben.ferreira@irbbarcelona.org |
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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. |
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