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Novel Sigma Binding Site Ligands as Inhibitors of Cell Proliferation in Breast Cancer

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Sigma receptors, namely σ1 and σ2, have been shown to be expressed in a variety of human cell lines playing a role in cell growth. In the human breast, they are absent in normal mammary tissue but expressed in tumors, particularly in the proliferating stage. The study presented here concerns nine newly synthesized ligands for sigma receptors. The compounds are of general structure consisting of: five (1α/1β-arylalkyl)quinolizidines including two thioisosteres and four spiro-[3,4-dihydro-1,2,4-benzotriazino-3,4′-(1′-substituted) piperidines]. These compounds exhibited varying degrees of affinity for sigma receptors and were able to inhibit the growth of MCF-7 and MDA-MB 231 human breast cancer cell lines, in vitro. Good to moderate binding to σ1 receptors occurred with all tested ligands. However, affinity for σ2 appeared more evident with compounds FN/C-2 and FN/C-4 (spiro-[3,4-dihydro-1,2,4-benzotriazino-3,4′-(1′-substituted) piperidines] derivatives). In addition, higher cytotoxic activity of FN/C-2 and FN/C-4 with IC50 values below 100 μM in MCF-7 and lower than 40 μM in MDA-MB 231 was revealed. The data from the current study show that these novel sigma receptor ligands exhibit interesting cytotoxic activity and suggest their potential for development as antitumor agents.

Keywords: Cytotoxic activity; MCF-7; MDA-MB 231; Sigma receptor ligands

Document Type: Research Article


Affiliations: 1: *Laboratory of Pharmacology and Neuroscience, National Institute for Cancer Research, Largo R. Benzi 10, 16132, Genoa, Italy 2: †Institute of Pharmaceutical Chemistry, University of Milan, Viale Abruzzi 42, 20131, Milan, Italy 3: ‡Department of Pharmaceutical Sciences, University of Genoa, Viale Benedetto XV, 3, 16132, Genoa, Italy

Publication date: 2003-01-01

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  • Formerly: Oncology Research Incorporating Anti-Cancer Drug Design
    Oncology Research Featuring Preclinical and Clincal Cancer Therapeutics publishes research of the highest quality that contributes to an understanding of cancer in areas of molecular biology, cell biology, biochemistry, biophysics, genetics, biology, endocrinology, and immunology, as well as studies on the mechanism of action of carcinogens and therapeutic agents, reports dealing with cancer prevention and epidemiology, and clinical trials delineating effective new therapeutic regimens.
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