• Título:  MOLÉCULAS PEQUEÑAS CONTENIENDO SELENIO COMO AGENTES ANTITUMORALES: SÍNTESIS Y DESARROLLO PRECLÍNICO
• Autor:  CALVO MARTIN, GORKA
• Universidad:  Universidad de Navarra
• Departamento:  Tecnología y química farmacéuticas
• Fecha de Lectura:  19/05/2022
• Programa de doctorado:  Programa de Doctorado en Medicamentos y Salud por la Universidad de Navarra
• Dirección: 
  • Sanmartín Grijalba, María del Carmen (DIRECTOR)
  • Plano Amatriain, Daniel (DIRECTOR)
• Tribunal: 
  • BUSTO SANCIRIÁN, JESÚS HECTOR (PRESIDENTE)
  • Moreno Amatria, Esther (SECRETARIO)
  • MARTÍNEZ MERINO, VÍCTOR (VOCAL)
  • AYDILLO MIGUEL, CARLOS (VOCAL)
  • ENCIO MARTINEZ, IGNACIO JOSE (VOCAL)
• Descriptores: 
  • QUIMICA DE LOS COMPUESTOS BICICLICOS
  • DISEÑO SINTESIS Y ESTUDIO DE NUEVOS FARMACOS
  • MECANISMOS DE LAS REACCIONES ORGANICAS
• Localización:  ARCHIVO DIGITAL UNIVERSIDAD DE NAVARRA
• Resumen:
  A series of novel selenium-containing compounds with potential antitumoral and/or leishmanicidal activity has been synthesized and evaluated in this work. Since the chemical form of selenium (Se) is determinant for its biological activity, we have explored the effects of different Se-containing substituents. To further increase the activity of the novel compounds, the different Se-containing substituents have been incorporated into different scaffolds which demonstrated antitumoral and antiparasitic activity. The novel derivatives containing the functionalities, methylseleno, selenocyanate, selenourea and diselenide have been tested against a panel of several human cancer cell lines. Some of these compound have been tested against Leishmania infantum amastigotes. The antioxidant capacity of selenoureas was also tested with outstanding results. Furthermore, three different cis-platin selenium containing compounds derived from the selenoureas were synthesized and tested in cancer cells and leishmania promastigotes. The central scaffold for most of the molecules synthesized was norbornene, a bicyclic structure derived from a Diels-Alder reaction. Those compounds containing norbornene were especially active against cancer cells in vitro. The ability of the Diels-Alder reaction to form bicycles was also tested with different dienes such as thiophene and selenophene, achieving the DA reaction of these dienes for the first time at atmospheric pressure in the presence a AlCl3. The most active and selective molecules in each case have been selected for further biological studies to elucidate their possible mechanism of action.