Publication: Derivados de Tiazolidina-2,4-dionas para el diseño de nuevos fármacos (II)
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2017-06
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Abstract
Los derivados de las Tiazolidina-2,4-dionas (TZD) son un grupo de fármacos compuestos por un anillo heterocíclico de tipo tiazol, es un núcleo heterocíclico muy explorado en el diseño de nuevas estructuras capaces de intervenir en una gran variedad de condiciones fisiopatológicas, como pueden ser la diabetes, las complicaciones derivadas de la misma, el cáncer, la artritis, la inflamación y el melanoma. Sin embargo, las propiedades más significativas son sus aplicaciones anticancerígenas indirectas al tratar la hiperinsulinemia característica de los pacientes con diabetes mellitus, y de otro tipo de mecanismos celulares más específicos, derivándose todos estos efectos en el paro del ciclo celular y a la inducción de la apoptosis en células tumorales. Los derivados de las TZD han demostrado en los últimos años la capacidad de suprimir el desarrollo tumoral tanto en estudios in Vitro como in Vivo. Dicha actividad reside en su acción sobre los receptores nucleares activados por proliferación del peroxisoma PPARγ, cuya activación mediante diversas rutas celulares, desencadena la apoptosis o muerte celular programada mediante la disminución de la insulina sistémica, entre otros procesos moleculares independientes del receptor PPARγ. Sin embargo, aunque dichas moléculas ofrezcan resultados convincentes, aun es necesaria la elaboración de más ensayos clínicos de terapia combinada. En este trabajo de fin de grado se llevará a cabo una rigurosa revisión bibliográfica sobre las diferentes características farmacológicas de las tiazolidinadionas, su mecanismo de acción, su síntesis y su repercusión en el organismo.
The derivatives of thiazolidine-2,4-diones (TZD) are a group of drugs composed of a thiazole-type heterocyclic ring, it is a highly explored heterocyclic nucleus in the design of new structures capable of intervening in a great variety of pathophysiological conditions, such as diabetes, complications derived from it, cancer, arthritis, inflammation and melanoma. However, the most significant properties are its indirect anticancer applications in treating the hyperinsulinemia characteristic of patients with diabetes mellitus, and of other types of more specific cellular mechanisms, all these effects being derived in the stop of the cell cycle and the induction of apoptosis In tumor cells. TZD derivatives have demonstrated in recent years the ability to suppress tumor development in both in vitro and in vivo studies. This activity resides in its action on nuclear receptors activated by peroxisome proliferation PPARγ, whose activation through various cellular pathways, triggers apoptosis or programmed cell death by decreasing systemic insulin, among other molecular processes independent of the PPARγ receptor. However, while such molecules offer convincing results, further clinical trials of combination therapy are still required. In this end-of-degree study, a rigorous bibliographic review will be carried out on the different pharmacological characteristics of thiazolidinediones, their mechanism of action, their synthesis and their repercussion in the organism.
The derivatives of thiazolidine-2,4-diones (TZD) are a group of drugs composed of a thiazole-type heterocyclic ring, it is a highly explored heterocyclic nucleus in the design of new structures capable of intervening in a great variety of pathophysiological conditions, such as diabetes, complications derived from it, cancer, arthritis, inflammation and melanoma. However, the most significant properties are its indirect anticancer applications in treating the hyperinsulinemia characteristic of patients with diabetes mellitus, and of other types of more specific cellular mechanisms, all these effects being derived in the stop of the cell cycle and the induction of apoptosis In tumor cells. TZD derivatives have demonstrated in recent years the ability to suppress tumor development in both in vitro and in vivo studies. This activity resides in its action on nuclear receptors activated by peroxisome proliferation PPARγ, whose activation through various cellular pathways, triggers apoptosis or programmed cell death by decreasing systemic insulin, among other molecular processes independent of the PPARγ receptor. However, while such molecules offer convincing results, further clinical trials of combination therapy are still required. In this end-of-degree study, a rigorous bibliographic review will be carried out on the different pharmacological characteristics of thiazolidinediones, their mechanism of action, their synthesis and their repercussion in the organism.