Quinazolinecarboline alkaloid evodiamine as scaffold for targeting topoisomerase I and sirtuins.


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.

DOI: 10.1016/j.bmc.2013.09.030

Cite this paper

@article{Christodoulou2013QuinazolinecarbolineAE, title={Quinazolinecarboline alkaloid evodiamine as scaffold for targeting topoisomerase I and sirtuins.}, author={Michael S. Christodoulou and Alessandro Sacchetti and Valentina Ronchetti and Stefania Caufin and Alessandra Silvani and Giordano Lesma and Gabriele Fontana and Fabrizio Minicone and Benedetta Riva and Micol Ventura and Maija Lahtela-Kakkonen and Elina M. Jarho and Valentina Zuco and Franco Zunino and Nadine Martinet and Federico Dapiaggi and Stefano Pieraccini and Maurizio Sironi and Lisa Dalla Via and Ornella Maria Gia and Daniele Passarella}, journal={Bioorganic & medicinal chemistry}, year={2013}, volume={21 22}, pages={6920-8} }