Journal
CHEMMEDCHEM
Volume 12, Issue 22, Pages 1893-1905Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201700427
Keywords
analgesia; antiproliferative activity; melanoma; sigma receptors; SK-MEL-2 cells
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Funding
- Fondazione Cassa di Risparmio di Modena [2015.0402]
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A new series of spirocyclic sigma receptor (sigma R) ligands were prepared and studied. Most were found to have a high affinity and selectivity for sigma R-1; three compounds were shown to be sigma R-1 agonists, while another proved to be the only sigma R-1 antagonist. Only one of the sigma R-1 agonists (BS148) also exhibited sigma R-2 selectivity and was able to inhibit the growth of metastatic malignant melanoma cell lines without affecting normal human melanocytes. The antiproliferative activity of this compound suggested an sigma R-2 agonist profile. Further, preliminary investigations indicated that the mechanism of metastatic malignant melanoma cell death induced by BS148 is due, at least in part, to apoptosis.
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