Synthesis, σ 1, σ 2-receptors binding affinity and antiproliferative action of new C1-substituted adamantanes

Autor: Riganas, S. Papanastasiou, I. Foscolos, G.B. Tsotinis, A. Bourguignon, J.-J. Serin, G. Mirjolet, J.-F. Dimas, K. Kourafalos, V.N. Eleutheriades, A. Moutsos, V.I. Khan, H. Georgakopoulou, S. Zaniou, A. Prassa, M. Theodoropoulou, M. Pondiki, S. Vamvakides, A.
Jazyk: angličtina
Rok vydání: 2012
Popis: The synthesis of N-4-[a-(1-adamantyl)benzyl]phenylpiperazines 2a-e is described. The in vitro antiproliferative activity of most compounds against main cancer cell lines is significant. The σ 1, σ 2-receptors and sodium channels binding affinity of compounds 2 were investigated. One of the most active analogs, 2a, had an interesting in vivo anticancer profile against the BxPC-3 and Mia-Paca-2 pancreas cancer cell lines with caspase-3 activation, which was associated with an anagelsic activity against the neuropathic pain. © 2012 Elsevier Ltd. All rights reserved.
Databáze: OpenAIRE