Data di Pubblicazione:
2016
Citazione:
4-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II / M.S. Christodoulou, M. Zarate, F. Ricci, G. Damia, S. Pieraccini, F. Dapiaggi, M. Sironi, L. Lo Presti, A.N. García Argáez, L. Dalla Via, D. Passarella. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 118:(2016), pp. 79-89. [10.1016/j.ejmech.2016.03.090]
Abstract:
The synthesis and biological evaluation of a new library of 4-(1,2-diarylbut-1-en-1-yl)isobutyranilides is described. The new compounds were found to be cytotoxic in the micromolar range in two human tumor cell lines, MCF-7 (mammary gland adenocarcinoma) and HeLa (cervix adenocarcinoma) and two human ovarian cancer cell lines (A2780 and OVCAR5). Detailed studies on the most active compound 6g show that it was able to induce apoptosis and suggest topoisomerase II as a possible intracellular target. The relevance of the interaction of the most active compound with topoisomerase II is demonstrated and supported by docking studies.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
McMurry reaction; tamoxifen derivatives; topoisomerase I and II; drug discovery3003 pharmaceutical science; organic chemistry; pharmacology
Elenco autori:
M.S. Christodoulou, M. Zarate, F. Ricci, G. Damia, S. Pieraccini, F. Dapiaggi, M. Sironi, L. Lo Presti, A.N. García Argáez, L. Dalla Via, D. Passarella
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