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Polydentate imine ligands as modulators of copper reactivity in inflammation-related diseases and in bioorthogonal coupling reactions

Grant number: 18/21537-6
Support type:Scholarships in Brazil - Post-Doctorate
Effective date (Start): January 01, 2019
Effective date (End): August 31, 2021
Field of knowledge:Physical Sciences and Mathematics - Chemistry - Inorganic Chemistry
Principal researcher:Ana Maria da Costa Ferreira
Grantee:Raphael Enoque Ferraz de Paiva
Home Institution: Instituto de Química (IQ). Universidade de São Paulo (USP). São Paulo , SP, Brazil
Associated research grant:13/07937-8 - Redoxome - Redox Processes in Biomedicine, AP.CEPID


In this project we will develop polydentate imine-derived ligands containing oxindole, imidazole and triazole moieties for stabilization of copper in both of its usual oxidation states in biological systems. These ligands will be investigated for two complementary applications. In one front, the polydentate ligands will be used for the synthesis of copper(II) metallodrugs aimed at the treatment of inflammation-related diseases. Copper has a central but dichotomic role related to inflammatory processes, involving reactive oxygen and/or nitrogen reactive species, as it has both pro- and anti-inflammatory properties. Furthermore, the correlation between cancer development and inflammation has become more and more clear, with a key aspect being the role of reactive oxygen and nitrogen species. That prompts us to investigate the fundamental role of copper in both processes. Based on our previous experience in studies of copper ion reactivity in biological medium, we intend to go further in our investigations on the possible mechanisms of action of potential antitumor agents based on copper, focusing on the link between cancer and inflammatory processes. Additionally, we intend to use the the polydentate imine-derived ligands as alternative co-ligands in the "click" copper(I)-catalyzed alcino-azide cycloaddition. Under the scope of Bioorthogonal Catalysis (catalysis in biological media), we aim at obtaining triazole-derived compounds with anticancer and fluorescent properties directly in aqueous media. Once these reactions are optimized, they can be translated to in cellulo and in vivo applications.

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Scientific publications (5)
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
ABRAO, FARIZA; SILVA, THAYNA SOUZA; MOURA, CLAUDIA L.; AMBROSIO, SERGIO RICARDO; SOLA VENEZIANI, RODRIGO CASSIO; DE PAIVA, RAPHAEL E. F.; BASTOS, JAIRO KENUPP; GOMES MARTINS, CARLOS HENRIQUE. Oleoresins and naturally occurring compounds of Copaifera genus as antibacterial and antivirulence agents against periodontal pathogens. SCIENTIFIC REPORTS, v. 11, n. 1 MAR 2 2021. Web of Science Citations: 0.
FERRAZ DE PAIVA, RAPHAEL ENOQUE; VIEIRA, EDUARDO GUIMARAES; RODRIGUES DA SILVA, DANIEL; WEGERMANN, CAMILA ANCHAU; COSTA FERREIRA, ANA MARIA. Anticancer Compounds Based on Isatin-Derivatives: Strategies to Ameliorate Selectivity and Efficiency. FRONTIERS IN MOLECULAR BIOSCIENCES, v. 7, FEB 4 2021. Web of Science Citations: 0.
DE PAIVA, RAPHAEL E. F.; NETO, ANTONIO MARCAL; SANTOS, IGOR A.; JARDIM, ANA C. G.; CORBI, PEDRO P.; BERGAMINI, FERNANDO R. G. What is holding back the development of antiviral metallodrugs? A literature overview and implications for SARS-CoV-2 therapeutics and future viral outbreaks. DALTON TRANSACTIONS, v. 49, n. 45, p. 16004-16033, DEC 7 2020. Web of Science Citations: 1.
DE PAIVA, RAPHAEL E. F.; PETERSON, ERICA J.; DU, ZHIFENG; FARRELL, NICHOLAS P. The leaving group in Au(I)-phosphine compounds dictates cytotoxic pathways in CEM leukemia cells and reactivity towards a Cys(2)His(2) model zinc finger. DALTON TRANSACTIONS, v. 49, n. 45, p. 16319-16328, DEC 7 2020. Web of Science Citations: 0.
FAZZI, RODRIGO B.; FERRAZ DE PAIVA, RAPHAEL E.; DA COSTA FERREIRA, ANA M. A combined EPR spectroscopy and DFT-based structural interpretation of the antitumor properties of oxindolimine-copper(II) complexes. ARKIVOC, n. 2, p. 123-133, 2020. Web of Science Citations: 0.

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