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  • About
  • The Global ETD Search service is a free service for researchers to find electronic theses and dissertations. This service is provided by the Networked Digital Library of Theses and Dissertations.
    Our metadata is collected from universities around the world. If you manage a university/consortium/country archive and want to be added, details can be found on the NDLTD website.
1

Compostos de paládio(II) contendo tiossemicarbazonas : síntese, interação com alvos enzimáticos e avaliação do potencial antitumoral /

Farias, Renan Lira de January 2020 (has links)
Orientador: Adriano Bof de Oliveira / Resumo: Prescrições semanais de 2 a 5 mg kg-1 de cisplatina tem oferecido um avanço no tratamento de vários tipos de cânceres geniturinários, sendo as taxas de sobrevida ca. 98%. Contudo, os complexos de Pt(II) se mostram inespecíficos frente às células normais de rápida proliferação, o que limita a dose a ser administrada. Nesta tese de doutorado, foram preparados oito complexos de Pd(II) do tipo [PdCl2(L)PPh3]Cl (família 1 a 4) e [Pd(L)2] (família 5 a 8), onde PPh3 = trifenilfosfina e L = trans-cinamaldeído-N4-R-tiossemicarbazona (R = H, Metila, Etila e Fenila). Os compostos foram caracterizados através das técnicas espectroscópicas de infravermelho com transformada de Fourier, ressonância magnética nuclear de 1H, 13C e 31P. As formulas mínimas e purezas dos compostos foram determinadas através de microanálise CHN%. Dados de condutância molar em DMF exibiram o perfil de eletrólito 1:1 para 1-4, enquanto os complexos 5 a 6 foram não eletrólitos. Os complexos 2, 3 e 6 formaram cristais aptos aos experimentos de difração de raios X por monocristal e obtiveram suas estruturas cristalinas resolvidas. Com o intuito de selecionar compostos líderes, ensaios in vitro de citotoxicidade e efeitos hemolíticos foram conduzidos como sequência de triagem. As respectivas citotoxicidades para todos os compostos foram investigadas pelo método colorimétrico MTT e expressas como CI50, frente às culturas tumorais humanas MCF-7 (adenocarcinoma mamário) e A549 (carcinoma de pulmão). Além disso, os índice... (Resumo completo, clicar acesso eletrônico abaixo) / Abstract: Weekly, prescriptions ranging at 2-5 mg kg-1 of cisplatin have offered an advance in the treatment of several genitourinary cancers, being survival rates ca. 98%. On the other hand, Pt(II) complexes are no selective in rapidly proliferating normal cells, which limits the dose to be administered. Herein, eight Pd (II) complexes of the type [PdCl2(L)PPh3]Cl (1-4) and [Pd(L)2] (5-8) were prepared (where, PPh3 = triphenylphosphine and L = trans-cinnamaldehyde-N4-R-thiosemicarbazone; R = H, Methyl, Ethyl and Phenyl). The compounds were characterized by using infrared and NMR 1H, 13C and 31P spectroscopic techniques. The minimum formula and purities of them were determined by using CHN% microanalysis. Molar conductivity data (at DMF) showed the electrolyte profile 1:1 to 1-4, while complexes 5-6 were non-electrolytes. Complexes 2, 3 and 6 formed suitable crystals for single-crystal X-ray diffraction experiments and their crystalline structures were solved. To select leading compounds, in vitro cytotoxicity and RBC hemolytic assays were performed out as a screening. For all compounds, the cytotoxicities were investigated by the MTT colourimetric method and expressed as IC50 in human tumour cultures MCF-7 (mammary adenocarcinoma) and A549 (lung carcinoma). Besides, selectivity index (IS) were estimated from the ratios between IC50 values against non-tumour cells MRC5 (lung fibroblast) and LLC-MK2 (Rhesus monkey kidney). Accordingly, three compounds were considered promising (L3, 3 an... (Complete abstract click electronic access below) / Doutor

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