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.
Evodiamine ; Quinazolinecarboline alkaloids ; Sirtuins ; Topoisomerase I ; enantiomer; ent ; epi ; epimer
Settore CHIM/06 - Chimica Organica
15-nov-2013
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/226383
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