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  3. In vitro studies on the inhibition of colon cancer by amino acid derivatives of bromothiazole

In vitro studies on the inhibition of colon cancer by amino acid derivatives of bromothiazole

  • Bioorg Med Chem Lett. 2017 Aug 1;27(15):3507-3510. doi: 10.1016/j.bmcl.2017.05.073.
Nuno Vale 1,  Ana Correia-Branco 2,  Bárbara Patrício 3,  Diana Duarte 4,  Fátima Martel 2
Affiliations

Affiliations

  • 1 UCIBIO/REQUIMTE, Department of Chemistry and Biochemistry, Faculty of Sciences of University of Porto, Rua do Campo Alegre, 687, 4169-007 Porto, Portugal; Laboratory of Pharmacology, Department of Drug Sciences, Faculty of Pharmacy of University of Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal. Electronic address: nuno.vale@fc.up.pt.
  • 2 Unit of Biochemistry, Department of Biomedicine, Faculty of Medicine of University of Porto, Alameda Professor Hernâni Monteiro, 4200-319 Porto, Portugal; i3S, University of Porto's Institute for Research and Innovation in Health, Rua Alfredo Allen, 208, 4200-135 Porto, Portugal.
  • 3 UCIBIO/REQUIMTE, Department of Chemistry and Biochemistry, Faculty of Sciences of University of Porto, Rua do Campo Alegre, 687, 4169-007 Porto, Portugal; Laboratory of Pharmacology, Department of Drug Sciences, Faculty of Pharmacy of University of Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal.
  • 4 UCIBIO/REQUIMTE, Department of Chemistry and Biochemistry, Faculty of Sciences of University of Porto, Rua do Campo Alegre, 687, 4169-007 Porto, Portugal; Laboratory of Pharmacology, Department of Drug Sciences, Faculty of Pharmacy of University of Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal; Unit of Biochemistry, Department of Biomedicine, Faculty of Medicine of University of Porto, Alameda Professor Hernâni Monteiro, 4200-319 Porto, Portugal.
PMID: 28601526 DOI: 10.1016/j.bmcl.2017.05.073
Abstract

The investment in Cancer research is critical to find more and better treatments, but essentially to save lives. Here, we describe the synthesis and characterization on new bromothiazole derivatives with Amino acids and with core of nitazoxanide, an FDA-approved antiprotozoal drug. Using a human adenocarcinoma-derived cell line (the Caco-2 cell line), we then investigated the antiproliferative (3H-thymidine incorporation) and cytotoxic (extracellular Lactate Dehydrogenase activity) effect of these derivatives. All the derivatives caused a concentration-dependent decrease in cell proliferation and viability. At their highest concentration, all compounds were able to reduce 3H-thymidine incorporation by more than 80%, corresponding to a more marked antiproliferative effect than butyrate. As to their cytotoxic effect, it was comparable to that of butyrate. The ability of bromo substituent in thiazole ring with new sequences of Amino acids in inducing cell death and Apoptosis in Caco-2 cells (and Other cell lines) is now being studied.

Keywords

(3)H-thymidine incorporation; Bromothiazole; Caco-2 cell; Colorectal cancer; Extracellular dehydrogenase activity.

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