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

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

  • Bioorg Med Chem Lett. 2017 Mar 1;27(5):1141-1144. doi: 10.1016/j.bmcl.2017.01.079.
Amalyn Nain-Perez 1,  Luiz C A Barbosa 2,  Diego Rodríguez-Hernández 1,  Annemarie E Kramell 3,  Lucie Heller 3,  René Csuk 4
Affiliations

Affiliations

  • 1 Department of Chemistry, Universidade Federal de Minas Gerais, Av. Pres. Antônio Carlos, 6627, Campus Pampulha, CEP 31270-901, Belo Horizonte, MG, Brazil.
  • 2 Department of Chemistry, Universidade Federal de Minas Gerais, Av. Pres. Antônio Carlos, 6627, Campus Pampulha, CEP 31270-901, Belo Horizonte, MG, Brazil; Department of Chemistry, Universidade Federal de Viçosa, Av. P.H. Rolfs, s/n, CEP 36570-900, Viçosa, MG, Brazil. Electronic address: lcab@ufmg.br.
  • 3 Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str.2, D 06120 Halle (Saale), Germany.
  • 4 Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str.2, D 06120 Halle (Saale), Germany. Electronic address: rene.csuk@chemie.uni-halle.de.
PMID: 28169163 DOI: 10.1016/j.bmcl.2017.01.079
Abstract

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 (2h-i) or a benzoyl group (3f-g), were the most potent against all human Cancer cell lines and displayed EC50 between a range of 0.6-3.4μM. Notably, of the compounds tested, compound 2i proved the most cytotoxic against both ovarian (A2780) and breast (MCF7) cells, showing EC50=0.6 and 0.8μM respectively. Likewise, the analogues 2i, 3f and 3g showed strong activity against cell HT29 with EC50=0.9μM for these compounds.

Keywords

Abenquines; Abenquines analogues; Aminoquinone; Cytotoxicity; SRB assay.

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