Synthesis and antiproliferative activity of novel selenoester derivatives

• 31 new selenoesters were synthesized and their cytotoxic activity was evaluated.
• Cancer cell lines evaluated: prostate (PC-3), breast (MCF-7), lung (A-549) and colon (HT-29).
• Cytotoxic, selectivity, cyclic voltammetry, GPx-like, DPPH activities were evaluated.
• In terms of GI50, compounds 3 and 13 were more potent than etoposide and cisplatin, respectively.

A series of 31 new selenoesters were synthesized and their cytotoxic activity was evaluated against a prostate cancer cell line (PC-3). The most active compounds were also tested against three tumoural cell lines (MCF-7, A-549 and HT-29) and one non-tumour prostate cell line (RWPE-1). Thirteen compounds showed significant activity towards all tumour cells investigated, and some of them were even more potent than etoposide and cisplatin, which were used as reference drugs. Because of their pronounced potency and/or selectivity, four analogues (5, 21, 28 and 30), were selected in order to assess their redox properties related to a possible redox modulating activity. The glutathione peroxidase (GPx) assay showed slight activity for compound 30 and the 2,2-diphenyl-1-picrylhydrazyl-(DPPH) assay showed a weak activity for compounds 5 and 28. The present results revealed that analogues 5, 21, 28 and 30 might serve as a useful starting point for the design of improved anti-tumour agents.

Modulation of selenoesters as antiproliferatives and redox actives.Figure optionsDownload as PowerPoint slide