Síntese, caracterização e investigação das atividades biológicas de compostos ciclopalados
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2013-04-19
Autores
Rogério, Ana Paula [UNESP]
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Universidade Estadual Paulista (Unesp)
Resumo
Os compostos de coordenação de paládio(II) possuem extensas aplicações nas mais diferentes áreas da química. Nos últimos anos, eles estão sendo cada vez mais estudados para catálise homogênea, química supramolecular, materiais líquidocristalinos e Medicina. Dentre esses compostos de paládio(II) destacam-se os ciclopaladados, por apresentarem em alguns casos atividade antitumoral comparável ou superior a da cisplatina e recentemente atividade antileishmanicida. Este trabalho teve como propósito sintetizar cinco novos complexos ciclopaladados mononucleares do tipo [PdCl(C2,N-bzox)L], onde bzox = benzaldeidooxima e L = tiouréia (1), N,N’-dimetiltiouréia (2),N-metiltiouréia (3), N-feniltiouréia (4) e tioacetamida (5) através de reações entre o precursor dimérico [Pd(μ-Cl)(C2,Nbzox)] 2 e os ligantes. Posteriormente os compostos foram caracterizados por Análise Elementar, Espectroscopia no IV (Infra-Vermelho), RMN (Ressonância Magnética Nuclear) e Espectrometria de Massas. Os complexos e a cisplatina tiveram sua citotoxicidade investigada, in vitro, pelo método do MTT frente à linhagem celular LM3 (adenocarcinoma mamário), onde os compostos 1, 2 e 4 apresentaram valores citotóxicos comparáveis a cisplatina. Os compostos também foram testados frente ao protozoário do gênero Leishmania e a concentração inibitória, IC50 foi determinada. O composto 4 com o ligante feniltiouréia mostrou-se o mais ativo com um IC50 de 1,56 μg mL-1, inclusive quando comparado a droga de referência Anfotericina B (IC50 = 6,95 μg mL-1)
Palladium (II) compounds been the subject of intense studies in various areas of chemistry, such as homogeneous catalysis, supramolecular chemistry, liquid crystalline materials and Bioinorganic chemistry. Among them, special attention has been devoted to palladacycles, because of their promising cytotoxic activity towards tumor cells as well their some cases they have antitumor activity comparable or superior to cisplatin and antileishmanicidal activity. This research aimed to synthesize five new mononuclear palladacycles complexes of the type [PdCl(C2,N-bzox)L], where bzox = benzaldeidooxima and L = thiourea (1), N,N’-dimethylthiourea (2), N-methylthiourea (3) N-phenylthiourea (4) and thioacetamide (5) through bridge splitting reaction between the dimeric precursor [Pd(μ-Cl)(C2,N-bzox)]2 and the ligands. Subsequently the compounds were characterized by Elemental Analysis, IR spectroscopy (Infra-Red), NMR (Nuclear Magnetic Resonance) and Mass Spectrometry. All the complexes and cisplatin have been tested in vitro by MTT assay for their cytotoxicity against the cell line LM3 (mammary adenocarcinoma), where the compounds 1, 2 and 4 showed to be as cytotoxic as cisplatin. The compounds were also tested against the Leishmania protozoa and the inhibitory concentration, IC50 was determined. Compound 4 with the ligand phenylthiourea proved to be the most active with an IC50 of 1.56 mg mL-1, even when compared to reference drug Amphotericin B (IC50 = 6.95 mg mL-1)
Palladium (II) compounds been the subject of intense studies in various areas of chemistry, such as homogeneous catalysis, supramolecular chemistry, liquid crystalline materials and Bioinorganic chemistry. Among them, special attention has been devoted to palladacycles, because of their promising cytotoxic activity towards tumor cells as well their some cases they have antitumor activity comparable or superior to cisplatin and antileishmanicidal activity. This research aimed to synthesize five new mononuclear palladacycles complexes of the type [PdCl(C2,N-bzox)L], where bzox = benzaldeidooxima and L = thiourea (1), N,N’-dimethylthiourea (2), N-methylthiourea (3) N-phenylthiourea (4) and thioacetamide (5) through bridge splitting reaction between the dimeric precursor [Pd(μ-Cl)(C2,N-bzox)]2 and the ligands. Subsequently the compounds were characterized by Elemental Analysis, IR spectroscopy (Infra-Red), NMR (Nuclear Magnetic Resonance) and Mass Spectrometry. All the complexes and cisplatin have been tested in vitro by MTT assay for their cytotoxicity against the cell line LM3 (mammary adenocarcinoma), where the compounds 1, 2 and 4 showed to be as cytotoxic as cisplatin. The compounds were also tested against the Leishmania protozoa and the inhibitory concentration, IC50 was determined. Compound 4 with the ligand phenylthiourea proved to be the most active with an IC50 of 1.56 mg mL-1, even when compared to reference drug Amphotericin B (IC50 = 6.95 mg mL-1)
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Química inorgânica, Cancer, Leishmaniose
Como citar
ROGÉRIO, Ana Paula. Síntese, caracterização e investigação das atividades biológicas de compostos ciclopalados. 2013. 88 f. Dissertação (mestrado) - Universidade Estadual Paulista Júlio de Mesquita Filho, Instituto de Química de Araraquara, 2013.