Literature DB >> 22512908

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

Stefanos Riganas1, Ioannis Papanastasiou, George B Foscolos, Andrew Tsotinis, Jean-Jacques Bourguignon, Guillaume Serin, Jean-François Mirjolet, Kostas Dimas, Vassilios N Kourafalos, Andreas Eleutheriades, Vassilios I Moutsos, Humaira Khan, Stavroula Georgakopoulou, Angeliki Zaniou, Margarita Prassa, Maria Theodoropoulou, Stavroula Pondiki, Alexandre Vamvakides.   

Abstract

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.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22512908     DOI: 10.1016/j.bmc.2012.03.038

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  3 in total

1.  Systemic delivery of gemcitabine triphosphate via LCP nanoparticles for NSCLC and pancreatic cancer therapy.

Authors:  Yuan Zhang; William Y Kim; Leaf Huang
Journal:  Biomaterials       Date:  2013-02-04       Impact factor: 12.479

Review 2.  Sigma Receptor (σR) Ligands with Antiproliferative and Anticancer Activity.

Authors:  Markos-Orestis Georgiadis; Olga Karoutzou; Angeliki-Sofia Foscolos; Ioannis Papanastasiou
Journal:  Molecules       Date:  2017-08-25       Impact factor: 4.411

3.  Biophysical Evaluation and In Vitro Controlled Release of Two Isomeric Adamantane Phenylalkylamines with Antiproliferative/Anticancer and Analgesic Activity.

Authors:  Marilena Vlachou; Angeliki-Sofia Foscolos; Angeliki Siamidi; Angeliki Syriopoulou; Nikitas Georgiou; Aikaterini Dedeloudi; Antonis D Tsiailanis; Andreas G Tzakos; Thomas Mavromoustakos; Ioannis P Papanastasiou
Journal:  Molecules       Date:  2021-12-21       Impact factor: 4.411

  3 in total

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