Natural abenquines and synthetic analogues: Preliminary exploration of their cytotoxic activity.
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 EC50between 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.
Department of Chemistry, Universidade Federal de Minas Gerais, Av. Pres. Antônio Carlos, 6627, Campus Pampulha, CEP 31270-901, Belo Horizonte, MG, Brazil.
Amalyn
A
Nain-Perez
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.
Luiz C A
LC
Barbosa
Department of Chemistry, Universidade Federal de Minas Gerais, Av. Pres. Antônio Carlos, 6627, Campus Pampulha, CEP 31270-901, Belo Horizonte, MG, Brazil.
Diego
D
Rodríguez-Hernández
Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str.2, D 06120 Halle (Saale), Germany.
Annemarie E
AE
Kramell
Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str.2, D 06120 Halle (Saale), Germany.
Lucie
L
Heller
Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str.2, D 06120 Halle (Saale), Germany. Electronic address: rene.csuk@chemie.uni-halle.de.
René
R
Csuk
D016475:3T3 Cells; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D051379:Mice; D011809:Quinones / Q000737:chemistry / Q000494:pharmacology*
D000970:Antineoplastic Agents; D011809:Quinones
Abenquines; Abenquines analogues; Aminoquinone; Cytotoxicity; SRB assay