Exploring the Biological Properties of Zn(II) thiosemicarbazone Helicates.
Sandra Fernández-Fariña, Isabel Velo-Heleno, Rocío Carballido, Miguel Martínez-Calvo, Ramiro Barcia, Òscar Palacios, Mercè Capdevila, Ana M González-Noya, Rosa Pedrido
Author Information
Sandra Fernández-Fariña: Departamento de Química Inorgánica, Facultade de Química, Campus Vida, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain. ORCID
Isabel Velo-Heleno: Departamento de Química Inorgánica, Facultade de Química, Campus Vida, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain. ORCID
Rocío Carballido: Departamento de Química Inorgánica, Facultade de Química, Campus Vida, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain.
Miguel Martínez-Calvo: Departamento de Química Inorgánica, Facultade de Química, Campus Vida, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain. ORCID
Ramiro Barcia: Departamento de Bioquímica y Biología Molecular, Facultade de Veterinaria, Campus Terra, Universidade de Santiago de Compostela, 27002 Lugo, Spain.
Òscar Palacios: Departament de Química, Universitat Autònoma de Barcelona, 08193 Cerdanyola del Vallès, Spain. ORCID
Mercè Capdevila: Departament de Química, Universitat Autònoma de Barcelona, 08193 Cerdanyola del Vallès, Spain. ORCID
Ana M González-Noya: Departamento de Química Inorgánica, Facultade de Química, Campus Vida, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain. ORCID
Rosa Pedrido: Departamento de Química Inorgánica, Facultade de Química, Campus Vida, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain.
The design of artificial helicoidal molecules derived from metal ions with biological properties is one of the objectives within metallosupramolecular chemistry. Herein, we report three zinc helicates derived from a family of thiosemicarbazone ligands with different terminal groups, Zn(L)∙2HO , Zn(L)∙2HO and Zn(L), obtained by an electrochemical methodology. These helicates have been fully characterized by different techniques, including X-ray diffraction. Biological studies of the zinc(II) helicates such as toxicity assays with erythrocytes and interaction studies with proteins and oligonucleotides were performed, demonstrating in all cases low toxicity and an absence of covalent interaction with the proteins and oligonucleotides. The in vitro cytotoxicity of the helicates was tested against MCF-7 (human breast carcinoma), A2780 (human ovarian carcinoma cells), NCI-H460 (human lung carcinoma cells) and MRC-5 (normal human lung fibroblasts), comparing the IC values with cisplatin. We will try to demonstrate if the terminal substituent of the ligand precursor exerts any effect in toxicity or in the antitumor activity of the zinc helicates.
