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Novos complexos mononucleares de Ga III e In III com ligantes não-simétricos

By Geovana Garcia Terra

Abstract

Tese (doutorado) - Universidade Federal de Santa Catarina, Centro de Ciências Físicas e Matemáticas, Programa de Pós-Graduação em Química, Florianópolis, 2012O crescente número de indivíduos que desenvolverão algum tipo câncer exige que sejam desenvolvidos radiofármacos e quimioterápicos seletivos, pois o diagnóstico preciso e um tratamento específico são fundamentais para a possibilidade de cura e da elevação da taxa de sobrevida. Motivados a tentar atender essas necessidades, neste trabalho tivemos como objetivo sintetizar e caracterizar novos complexos mononucleares de GaIII e InIII com ligantes não-simétricos, NO-doadores, hexadentados inéditos, sendo os complexos potenciais radiofármacos e/ou quimioterápicos. Foram obtidos 8 complexos mononucleares de GaIII e de InIII. Os complexos foram caracterizados utilizando-se as técnicas de análise elementar, espectroscopia de infravermelho, ressonância magnética nuclear de 1H, espectrometria de massas, condutivimetria e utilizou-se para os complexos GaL1, InL1, GaL2 e InL5 a difração de raios x para determinar a estrutura cristalina. Todos os complexos de Ga e In obtidos, tiveram sua estabilidade em solução avaliada a partir de coletas de espectros de RMN 1H, em DMSO-d6, nas temperaturas de 22, 36 e 55°C; sendo observado que os complexos são estáveis em solução. A citotoxicidade dos ligantes e complexos foi avaliada frente a células leucêmicas e os resultados revelaram que os complexo são ativos em concentrações a partir de 2,5 ?M, e os ligantes testados também apresentaram citoxicidade a partir de 5,0 ?M. Além disso, todos os compostos induziram a morte celular por apoptose. O fato de as concentrações necessárias para atingir o IC50 serem superiores às utilizadas em radiofarmácia indica que todos os complexos são potenciais radiofármacos.<br>Abstract : The growing number of individuals who will develop some type of cancer require selective radiopharmaceutical and chemotherapeutic agents for accurate diagnosis associated with a specific treatment. The combination of these factors is fundamental for the possibility of cure and raising the survival rate. In and Ga elements stand out in their use as radionuclides (67Ga, 111In, and 68Ga) to obtain radiopharmaceutical used in imaging techniques such as PET and SPECT. Promising results from studies of complex GaIII have boosted interest in this metal-based chemotherapy. InIII have already been described as a potential agent against bacteria and cancer. Motivated by the need to obtain more effective and selective radiopharmaceuticals and chemotherapy, in this work we describe the synthesis and characterization (by infrared spectroscopy, and nuclear magnetic resonance 1H and 13C) of 5 novel ligands mononucleates hexadentate unsymmetrical suitable for obtaining complexes with the cations and GaIII InIII stable under physiological conditions. GaIII and InIII were obtained as complexs with the ligands HL1, H2L2, H3L3 and HL5, and HL1 was also obtained as a complex with Fe. The complexes were characterized by elementar analysis, infrared spectroscopy, nuclear magnetic resonance 1H, mass spectrometry, conductivity measurement and for GaL1, InL1, GaL2 and InL5 complexes x-ray diffraction was also used to determine the crystalline structures. For all complexes obtained, except FeHL1, stability was evaluated in solution from collections of 1H NMR spectra at temperatures of 22, 36 and 55°C; it was observed that the complexes are stable in solution. The cytoxic activity was evaluated for all complexes and ligands in leukemic cells and the results showed that only FeL1 complex is inactive, and the others are active at concentrations from of 5 ìM. Furthermore, all compounds induced cell death by apoptosis. The fact that the concentrations needed to achieve the IC50 are greater than that used in radiopharmacy indicates that all complexes are potential radiopharmaceuticals

Topics: Quimica, Galio, Agentes antineoplasicos, Cancer -, Quimioterapia, Radioterapia, Cancer -, Tratamento, Medicina nuclear
Year: 2012
OAI identifier: oai:agregador.ibict.br.RI_UFSC:oai:repositorio.ufsc.br:123456789/100585
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