Natural abenquines and synthetic analogues: Preliminary exploration of their cytotoxic activity

• Author(s): Nain-Perez, Amalyn ; Barbosa, Luiz C.A. ; Rodríguez-Hernández, Diego ; Kramell, Annemarie E. ; Heller, Lucie ; Csuk, René
• Date: 2018
• Origin: Oasisbr
• Subject(s): Abenquines; Aminoquinone; Abenquines analogues; Cytotoxicity; SRB assay
• Document Type: Journal article
• Language: English

Description

In this study, we explore the cytotoxic activity of four natural abenquines (2a–d) and fourteen synthetic analogues (2e–j and 3a–h) against a panel of six human cancer cell lines using a SRB assay. It was found that most of the compounds revealed higher levels of cytotoxic activities than naturally occurring abenquines. The analogues carrying ethylpyrrolidinyl and ethylpyrimidinyl with either an acetyl group (2 h–i) or a benzoyl group (3f–g), were the most potent against all human cancer cell lines and displayed EC50 between a range of 0.6–3.4 μM. Notably, of the compounds tested, compound 2i proved the most cytotoxic against both ovarian (A2780) and breast (MCF7) cells, showing EC50 = 0.6 and 0.8 μM respectively. Likewise, the analogues 2i, 3f and 3 g showed strong activity against cell HT29 with EC50 = 0.9 μM for these compounds.