Synthesis of new heteropolycyclic compounds with potential antitumor activity = Preparació de nous compostos fenólics i derivats amb potencial activitat antitumoral

• Autores: Richard Soucek
• Directores de la Tesis: Maria Dolors Pujol Dilme (dir. tes.)
• Lectura: En la Universitat de Barcelona ( España ) en 2014
• Idioma: inglés
• Tribunal Calificador de la Tesis: Jaime Rubio Martínez (presid.), Jordi Morral Cardoner (secret.), Daniel-henry Caignard (voc.)
• Materias:
  • Química
    • Química orgánica
      • Compuestos heterocíclicos
  • Ciencias médicas
    • Ciencias clínicas
      • Oncología
• Enlaces
  • Tesis en acceso abierto en:  TDX  Dipòsit Digital de la UB 
• Resumen

  • The study deals with the synthesis and biological activity of 4 different antitumours: Tetrahydro-[1,4]-dioxanisoquinolines, combretastatin A-4, dioxancarbazoles and resveratrol analogues. This study describes the synthesis strategy and multi-step synthesis of these potential antitumour compounds. Various tetrahydroisoquinolines were synthesized, five of which were biologically tested and have a promising K-Ras inhibition activity. Two of them show a high antiangiogenesis activity, one of which also presents antiosteoporosis properties. Two pirazolone derivatives were synthetized and biologically tested, one of which shows a very high K-Ras inhibition, antiangiogenesis and antiosteoporosis activity and inhibits the G2 cell cycle phases and subphases. Two azoledione combretastatin A-4 derivatives were also synthesized and will be biologically tested. Two dioxancarbazoles were prepared and biologically tested, one of which shows a high K-Ras and angiogenesis inhibition. Finally, four resveratrol analogues were synthesized and biologically tested. Their biological results show a moderate and selective K-Ras inhibition on the studied cell lines. In the future, the rest of the synthesized compounds are to be biologically tested. Further CDKs and topoisomerase II inhibition trials as well as toxicity studies will be carried out.