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.
Quinazolinecarboline alkaloid evodiamine as scaffold for targeting topoisomerase I and sirtuins / M.S. Christodoulou, A. Sacchetti, V. Ronchetti, S. Caufin, A. Silvani, G. Lesma, G. Fontana, F. Minicone, B. Riva, M. Ventura, M. Lahtela Kakkonen, E. Jarho, V. Zuco, F. Zunino, N. Martinet, F. Dapiaggi, S. Pieraccini, M. Sironi, L. Dalla Via, O.M. Gia, D. Passarella. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 21:22(2013 Nov 15), pp. 6920-6928. [10.1016/j.bmc.2013.09.030]
Quinazolinecarboline alkaloid evodiamine as scaffold for targeting topoisomerase I and sirtuins
M.S. Christodoulou;A. Silvani;G. Lesma;G. Fontana;F. Dapiaggi;S. Pieraccini;M. Sironi;D. Passarella
2013
Abstract
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.
Pubblicazioni consigliate
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
