Synthesis, σ1, σ2-receptors binding affinity and antiproliferative action of new C1-substituted adamantanes

Autor:	Andrew Tsotinis, Margarita Prassa, Guillaume Serin, Ioannis Papanastasiou, Humaira Khan, Stavroula Georgakopoulou, Vassilios I. Moutsos, Jean-Jacques Bourguignon, Jean-François Mirjolet, Vassilios N. Kourafalos, Angeliki Zaniou, Alexandre Vamvakides, Stavroula Pondiki, Stefanos Riganas, Andreas Eleutheriades, George B. Foscolos, Kostas Dimas, Maria Theodoropoulou
Rok vydání:	2012
Předmět:	Stereochemistry Chemistry Sodium channel Organic Chemistry Clinical Biochemistry Pharmaceutical Science Biochemistry In vitro Cell culture In vivo Drug Discovery Molecular Medicine Inhibitory concentration 50 Molecule Cancer cell lines Receptor Molecular Biology
Zdroj:	Bioorganic & Medicinal Chemistry. 20:3323-3331
ISSN:	0968-0896
Popis:	The synthesis of N-{4-[a-(1-adamantyl)benzyl]phenyl}piperazines 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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::f08a918951df6498e0fc5e76bc3786e4 https://doi.org/10.1016/j.bmc.2012.03.038 Zobrazit plný text záznamu Full Text from ScienceDirect