TY - JOUR
TI - New adamantane derivatives with sigma affinity and antiproliferative activity
AU - Riganas, S.
AU - Papanastasiou, I.
AU - Foscolos, G.B.
AU - Tsotinis, A.
AU - Dimas, K.
AU - Kourafalos, V.N.
AU - Eleutheriades, A.
AU - Moutsos, V.I.
AU - Khan, H.
AU - Margarita, P.
AU - Georgakopoulou, S.
AU - Zaniou, A.
AU - Theodoropoulou, M.
AU - Mantelas, A.
AU - Pondiki, S.
AU - Vamvakides, A.
JO - RSC Medicinal Chemistry
PY - 2012
VL - 8
TODO - 4
SP - 569-586
PB - 
SN - null
TODO - 10.2174/157340612801216201
TODO - 4 (1 adamantyl) 4,4 diarylbutylamine;  5 (1 adamantyl) 5,5 diarylpentylamine;  6 (1 adamantyl) 6,6 diarylhexylamine;  adamantane derivative;  alkene;  methanol;  sigma opiate receptor;  sodium channel;  unclassified drug, animal cell;  antineoplastic activity;  antiproliferative activity;  article;  binding affinity;  cancer cell;  drug binding;  human;  human cell;  in vitro study;  in vivo study;  mouse;  nonhuman;  priority journal, Adamantane;  Animals;  Antineoplastic Agents;  Binding Sites;  Cell Line, Tumor;  Cell Proliferation;  Drug Design;  Female;  Humans;  Male;  Mice;  Mice, SCID;  Neoplasms;  Receptors, sigma
TODO - The synthesis of 4-(1-adamantyl)-4,4-diarylbutylamines 1, 5-(1-adamantyl)-5,5-diarylpentylamines 2 and 6-(1-adamantyl)-6,6- diarylhexylamines 3 is described and the σ1, σ2-receptors and sodium channels binding affinity of compounds 1 were investigated. The in vitro activity of compounds 1, 2 and 3 against main cancer cell lines is significant. One of the most active analogs, 1a, had an interesting in vivo anticancer profile against the ovarian cancer cell line IGROV-1, which was associated with an anagelsic activity against the neuropathic pain induced by the main anticancer drugs. © 2012 Bentham Science Publishers.
ER -