This paper reports the synthesis of a series of evodiamine derivatives. We assayed the ability to inhibit cell growth on three human tumour cell lines (H460, MCF-7 and HepG2) and we evaluated the capacity to interfere with the catalytic activity of topoisomerase I both by the relaxation assay and the occurrence of the cleavable complex. Moreover, whose effect on sirtuins 1, 2 and 3 was investigated. Finally, molecular docking analyses were performed in an attempt to rationalize the biological results.
|Titolo:||Quinazolinecarboline alkaloid evodiamine as scaffold for targeting topoisomerase I and sirtuins|
|Parole Chiave:||Evodiamine ; Quinazolinecarboline alkaloids ; Sirtuins ; Topoisomerase I ; enantiomer; ent ; epi ; epimer|
|Settore Scientifico Disciplinare:||Settore CHIM/06 - Chimica Organica|
|Data di pubblicazione:||15-nov-2013|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1016/j.bmc.2013.09.030|
|Appare nelle tipologie:||01 - Articolo su periodico|