751d52264855d20aa9fbb54eec333c7a pmc_9916454.pdf 8b0a14b95eea9b835d76593a3a6678374f60a84d pmc_9916454.pdf d96c42e0629622aff5d7e71e017ab65f1cfd638c2938fd4fa125550c9d460b2a pmc_9916454.pdf Title: Exploring the Biological Properties of Zn(II) Bisthiosemicarbazone Helicates Subject: 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 bisthiosemicarbazone ligands with different terminal groups, Zn2(LMe)22H2O 1, Zn2(LPh)22H2O 2 and Zn2(LPhNO2)2 3, 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 IC50 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. Keywords: bisthiosemicarbazone ligands; zinc; helicates; biological activity Author: Sandra Fernández-Fariña, Isabel Velo-Heleno, Rocío Carballido, Miguel Martínez-Calvo, Ramiro Barcia, Òscar Palacios, Mercè Capdevila, Ana M. González-Noya and Rosa Pedrido Creator: LaTeX with hyperref Producer: pdfTeX-1.40.21 CreationDate: Mon Jan 23 10:28:33 2023 CET ModDate: Mon Jan 23 10:38:54 2023 CET Tagged: no UserProperties: no Suspects: no Form: none JavaScript: no Pages: 16 Encrypted: no Page size: 595.276 x 841.89 pts (A4) Page rot: 0 File size: 5332570 bytes Optimized: no PDF version: 1.7 name type encoding emb sub uni object ID ------------------------------------ ----------------- ---------------- --- --- --- --------- QNEOQK+VnURWPalladioL Type 1 Custom yes yes no 10 0 GTPECH+URWPalladioL-Bold Type 1 Custom yes yes no 15 0 SXXLPE+URWPalladioL-Roma Type 1 Custom yes yes no 20 0 MJQUNF+URWPalladioL-Ital Type 1 Custom yes yes no 24 0 FLMPPG+URWPalladioL-BoldItal Type 1 Custom yes yes no 28 0 LKDISN+CMSY10 Type 1 Builtin yes yes no 32 0 USGSTI+VnURWPalladioL-Bold Type 1 Custom yes yes no 36 0 IRWHZX+TimesNewRomanPSMT Type 1C WinAnsi yes yes no 54 0 CKUPDE+TimesNewRomanPS-BoldItalicMT Type 1C WinAnsi yes yes no 57 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Size: 5332570 Format: PDF Version: 1.7 Status: Well-Formed and valid SignatureMatches: PDF-hul MIMEtype: application/pdf PDFMetadata: Objects: 501 FreeObjects: 1 IncrementalUpdates: 0 DocumentCatalog: PageLayout: SinglePage PageMode: UseNone Outlines: Item: Title: Introduction Destination: section.1 Item: Title: Results and Discussion Destination: section.2 Children: Item: Title: Synthesis and Characterization of the Ligands H2LMe, H2LPh and H2LPhNO2 Destination: subsection.2.1 Item: Title: Synthesis and Characterization of the Zinc Helicates Destination: subsection.2.2 Item: Title: Toxicity Assays Destination: subsection.2.3 Item: Title: Interaction with Proteins and Oligonucleotides Destination: subsection.2.4 Item: Title: Cytotoxicity Studies Destination: subsection.2.5 Item: Title: Materials and Methods Destination: section.3 Children: Item: Title: Synthesis and Characterization of Precursor PCDA and the Ligands H2LMe, H2LPh and H2LPhNO2 Destination: subsection.3.1 Item: Title: Synthesis and Characterization of the Zinc(II) Helicates Destination: subsection.3.2 Item: Title: X-ray Crystallography Destination: subsection.3.3 Item: Title: Toxicity Assays Destination: subsection.3.4 Children: Item: Title: Extraction and Culture Destination: subsubsection.3.4.1 Item: Title: Cell Viability Assessment Destination: subsubsection.3.4.2 Item: Title: Toxicity Studies Destination: subsubsection.3.4.3 Item: Title: Statistical Analysis Destination: subsubsection.3.4.4 Item: Title: Interactions with Proteins and Oligonucleotides Studies Destination: subsection.3.5 Item: Title: Citotoxicity Studies Destination: subsection.3.6 Item: Title: Conclusions Destination: section.4 Item: Title: References Destination: section.4 Info: Title: Exploring the Biological Properties of Zn(II) Bisthiosemicarbazone Helicates Author: Sandra Fernández-Fariña, Isabel Velo-Heleno, Rocío Carballido, Miguel Martínez-Calvo, Ramiro Barcia, Òscar Palacios, Mercè Capdevila, Ana M. González-Noya and Rosa Pedrido Subject: 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 bisthiosemicarbazone ligands with different terminal groups, Zn2(LMe)22H2O 1, Zn2(LPh)22H2O 2 and Zn2(LPhNO2)2 3, 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 IC50 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. 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