Τίτλος:
Synthesis, σ 1, σ 2-receptors binding affinity and antiproliferative action of new C1-substituted adamantanes
Γλώσσες Τεκμηρίου:
Αγγλικά
Περίληψη:
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.
Συγγραφείς:
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.
Περιοδικό:
BIOORGANIC AND MEDICINAL CHEMISTRY
Λέξεις-κλειδιά:
1 [4 [alpha (1 tricyclo[3.3.1.1 3,7]decyl)phenylmethyl]phenyl]piperazine; 1 cyclohexyl 4 [4 [alpha (1 tricyclo[3.3.1.1 3,7]decyl)phenylmethyl]phenyl]piperazine; 1 ethyl 4 [4 [alpha (1 tricyclo[3.3.1.1 3,7]decyl)phenylmethyl]phenyl]piperazine; 1 methyl 4 [4 [alpha (1 tricyclo[3.3.1.1 3,7]decyl)phenylmethyl]phenyl]piperazine; 1 methyl 4 [alpha,a diphenyl(1 tricyclo[3.3.1.1 3,7]decyl)methyl]piperazine; 1 phenylmethyl 4 [4 [alpha (1 tricyclo[3.3.1.1 3,7]decyl)phenylmethyl]phenyl]piperazine; 1 phenylmethyl 4 [alpha,a diphenyl(1 tricyclo[3.3.1.1 3,7]decyl)methyl]piperazine; 4 [4 [alpha (1 tricyclo[3.3.1.1 3,7]decyl)phenylmethyl]phenyl]morpholine; 4 [a,alpha diphenyl (1 tricyclo[3.3.1.1 3,7]decyl)methyl]morpholine; amantadine derivative; caspase 3; fluorouracil; gabapentin; gemcitabine; paclitaxel; piperazine derivative; sigma 1 opiate receptor; sigma 2 opiate receptor; sodium channel; unclassified drug, analgesic activity; animal experiment; animal model; antiproliferative activity; article; binding affinity; cancer cell; controlled study; drug cytotoxicity; drug design; drug screening; drug structure; drug synthesis; female; human; human cell; in vitro study; in vivo study; male; mouse; multiple cycle treatment; neuropathic pain; nonhuman; pancreas cancer; tumor xenograft, Adamantane; Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Humans; Inhibitory Concentration 50; Mice; Mice, Nude; Molecular Structure; Pancreatic Neoplasms; Receptors, sigma, Agouti paca
DOI:
10.1016/j.bmc.2012.03.038
