RESUMO
Se realiza una revisión poniendo foco en la fase de recuperación de la prueba ergométrica graduada, utilizando un caso clínico como punto de partida. Comenzamos con una síntesis de los fenómenos fisiológicos que operan durante esta etapa y se analizan las complicaciones, principalmente arritmias, definiendo su valor diagnóstico y pronóstico. Se concluye con una recomendación sobre cuándo es pertinente la finalización de la prueba.
Assuntos
Humanos , Ergometria/métodos , Ergometria/normasRESUMO
In the search for new potentially anticancer drugs, series of angucyclinone aza-analogues containing pyridine and pyridopyridazine rings have been designed and synthesized by a highly efficient sequence involving a one-pot step for the synthesis of tricyclic quinone intermediate and highly regiocontrolled cycloaddition reactions with polarized 1,3-dienes. The new N-heterocyclic angular quinones were evaluated in vitro on normal human fibroblasts and on a panel of four distinct human cancer cell lines. All tested compounds showed high to moderate antitumor activity. Among the compounds, those with one and two pyridine moieties fused to the quinone system have shown the best effect. Structure-activity relationships established the main structural requirement for the activity of the new potential anticancer drugs.
Assuntos
Antraquinonas/química , Antraquinonas/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Antraquinonas/síntese química , Antineoplásicos/síntese química , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Concentração Inibidora 50 , Células Tumorais CultivadasRESUMO
In the search for new potentially anticancer drugs, isoquinolinequinone-containing polycyclic compounds have been designed and synthesized through highly regiocontrolled cycloaddition reactions of methyl 1,3-dimethyl-5,8-dioxo-5,8-dihydroisoquinoline-4-carboxylate with polarized 1,3-dienes and a thiazole-o-quinodimethane. The new N-heterocyclic quinones were tested on normal human fibroblasts and four distinct human cancer cell lines. Two of the evaluated compounds displayed significant in vitro activity (IC50: 0.44-5.9 microM) comparable to that of the reference drug etoposide.
Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Quinonas/síntese química , Quinonas/farmacologia , Antineoplásicos/química , Linhagem Celular , Linhagem Celular Tumoral , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Etoposídeo/farmacologia , Fibroblastos/efeitos dos fármacos , Humanos , Quinonas/químicaRESUMO
Acylhydroquinone-based compounds are attractive targets for the design of new leishmanicidal drugs. We have previously described sesquiterpene quinones and hydroquinones series, which exhibit different degree of potency against Leishmania amazonensis. The present study details the preparation of acylchloroquinones and hydroquinones possessing lipophilic substituents and examines their in vitro activity against intracellular L. amazonensis amastigotes. The quinone or hydroquinone nucleus is essential for the activity of the members of the series. The lipophilicity of the cycloaliphatic systems in these members seems to attenuate the cytotoxical effect and increases the selectivity of those compounds containing the norbornene system.
