Τίτλος:
New adamantane derivatives with sigma affinity and antiproliferative activity
Γλώσσες Τεκμηρίου:
Αγγλικά
Περίληψη:
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.
Συγγραφείς:
Riganas, S.
Papanastasiou, I.
Foscolos, G.B.
Tsotinis, A.
Dimas, K.
Kourafalos, V.N.
Eleutheriades, A.
Moutsos, V.I.
Khan, H.
Margarita, P.
Georgakopoulou, S.
Zaniou, A.
Theodoropoulou, M.
Mantelas, A.
Pondiki, S.
Vamvakides, A.
Περιοδικό:
RSC Medicinal Chemistry
Λέξεις-κλειδιά:
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
DOI:
10.2174/157340612801216201
