Avances recientes en el diseño de complejos de platino con actividad antitumoral
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2019-06-12
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Jaén: Universidad de Jaén
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[ES] En este TFG se revisan los aspectos más relevantes del platino, especialmente aquellos relacionados con su química de la coordinación. Se describen las aplicaciones que tienen en medicina algunos complejos de platino con actividad antitumoral, entre los que destaca el cis-platino, primer fármaco de platino empleado a nivel clínico como agente anticancerígeno. Se enuncian las principales reglas estructura-actividad sobre las que se inició la búsqueda de nuevos fármacos antitumorales de platino. Se describe cómo se han ido desarrollando nuevas generaciones de fármacos anticancerígenos de platino. Finalmente, se presentan los últimos avances en el diseño de fármacos de platino antitumorales que se han llevado a cabo siguiendo las siguientes líneas de trabajo: i) diseño de complejos de platino con nuevos modos de unión al ADN, ii) diseño de complejos de platino dirigidos específicamente a moléculas "diana" presentes en células cancerígenas, iii) diseño de complejos de platino(IV) que actúen como profármacos
[EN] In this Final Degree Project, a review of the most relevant aspects of platinum is presented, specially those related to its coordination chemistry. The applications that have in medicine sorne antitumoral platinum complexes are described, among which cis-platinum, the first platinum drug used clinically as an anticancer agent, stands out. The main structure-activity rules are listed below, on which the search for new platinum antitumor drugs began. lt is described how new generations of platinum anticancer drugs have been developed over the last decades. Finally, we present the latest advances in the design of platinum drugs with antitumor activity that have been carried out following the following lines of work: i) design of platinum complexes that present new modes of DNA binding, ii) design of platinum complexes specifically targeted to "target" molecules present in cancer cells, iii)design of platinum (IV) complexes that actas prodrugs.
[EN] In this Final Degree Project, a review of the most relevant aspects of platinum is presented, specially those related to its coordination chemistry. The applications that have in medicine sorne antitumoral platinum complexes are described, among which cis-platinum, the first platinum drug used clinically as an anticancer agent, stands out. The main structure-activity rules are listed below, on which the search for new platinum antitumor drugs began. lt is described how new generations of platinum anticancer drugs have been developed over the last decades. Finally, we present the latest advances in the design of platinum drugs with antitumor activity that have been carried out following the following lines of work: i) design of platinum complexes that present new modes of DNA binding, ii) design of platinum complexes specifically targeted to "target" molecules present in cancer cells, iii)design of platinum (IV) complexes that actas prodrugs.