RESUMO
In this work, 22 new compounds were obtained and evaluated for their cytotoxic activity on peripheral blood mononuclear cells (PBMC) and eight different tumor cell lines. All compounds displayed IC50 values above 100 µM when assayed against PBMCs. The cytotoxic assays in tumor cell lines revealed that sub-series of phthalimido-bis-1,3-thiazoles (5a-f) exhibited the best anti-tumor activity profile, presenting viability values below 59 %. As a result, the IC50 value was calculated for compounds 5a-f and 4c, and compounds 5b and 5e were selected for further assays due to their best IC50s. Considering the results presented by the sub-series 5a-f, the importance of the 1,3-thiazole ring in improving the anti-tumor activity was pointed out. Together, the results highlighted the anti-tumor activity of phthalimido-bis-1,3-thiazole derivatives.
Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Tiazóis/síntese química , Tiazóis/farmacologia , Linhagem Celular , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Células HL-60 , Humanos , Células K562 , Leucócitos Mononucleares/efeitos dos fármacos , Estrutura Molecular , Relação Estrutura-AtividadeRESUMO
A cross-sectional study of secondary data/information obtained from the Hospital Information System (HIS) spanning the years 2008 - 2009 was performed. The distribution of the main hospital admissions by gender, age, color/race, region and federal unit of residence, average expenditure and average length of hospital stay, year of hospitalization and mortality rates (MR) were studied. The data collected were tabulated by TabNet and keyed into Microsoft Excel 2007. It was verified that elderly males (54.3%), from 60 to 69 years old (50.6%), nonwhites (36.3%) and residents of Southeast and North regions of the country had the highest rates of hospitalization. Seniors were hospitalized for an average of 4.8 days, and the major causes were exposure to alcohol (43.7%) and to drugs (33.9%). Expenses related to hospital admissions were, on average, R$ 529,817.70. The highest mortality rates were recorded among females (MR = 4.34), in elderly, 80 years or older (MR = 10.16) and Caucasians (MR = 3.95), where pharmacological substances with action on the Autonomic Nervous System were the leading cause of death. There are demographic differences in morbi-mortality of these elderly since, although men and younger elderly were the main victims, women and elderly of advanced age have greater mortality. The leading causes of hospitalization were alcohol and drugs.
Realizou-se um estudo transversal de dados secundários obtidos no Sistema de Informação Hospitalar (SIH), nos anos 2008/2009. Estudou-se a distribuição das principais internações segundo sexo; faixa etária; cor/raça; região e unidade federativa de residência; valor médio pago e média de permanência das internações hospitalares; ano de internação e as taxas de mortalidade (TM). Os dados coletados foram tabulados por meio do TabNet e transcritos para o Programa Microsoft Excel® 2007. Verificou-se que idosos do sexo masculino (54,3%), com 60 e 69 anos de idade (50,6%), não brancos (36,3%) e residentes nas regiões Sudeste e Norte do País apresentaram os maiores percentuais de internação hospitalar. Idosos ficam em média 4,8 dias internados, sendo as principais causas a exposição ao álcool (43,7%) e a medicamentos (33,9%). Os gastos com as internações equivaleram a R$ 529.817,70. As maiores taxas de mortalidade foram registradas no sexo feminino (TM=4,34), em idosos entre 80 anos e superior (TM=10,16) e pessoas brancas (TM=3,95), sendo as substâncias farmacológicas de ação sobre o Sistema Nervoso Autônomo maiores causas do óbito. Existem diferenças demográficas na morbimortalidade desses idosos, visto que apesar de homens e idosos mais jovens serem as principais vítimas, mulheres e idosos com idade mais avançada morrem mais. Sendo as principais causas de internação o álcool e os medicamentos.
