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Inicio  /  Cancers  /  Vol: 12 Par: 11 (2020)  /  Artículo
ARTÍCULO
TITULO

Sunitinib-Containing Carborane Pharmacophore with the Ability to Inhibit Tyrosine Kinases Receptors FLT3, KIT and PDGFR-ß, Exhibits Powerful In Vivo Anti-Glioblastoma Activity

Catalina Alamón    
Belén Dávila    
María Fernanda García    
Carina Sánchez    
Mariángeles Kovacs    
Emiliano Trias    
Luis Barbeito    
Martín Gabay    
Nidal Zeineh    
Moshe Gavish    
Francesc Teixidor    
Clara Viñas    
Marcos Couto and Hugo Cerecetto    

Resumen

Glioblastoma is one of the most aggressive central nervous system tumors. Combinations of therapies, such as tyrosine kinase receptor inhibition and boron neutron capture therapy (BNCT), could offer greater patients benefits over single-therapies. The aim of our study was to assess the potential of sunitinib-carborane hybrid compound 1 as an anti-glioblastoma agent. We confirmed for 1 the ability to inhibit tyrosine kinase receptors, which could promote canonical and non-canonical effects, absence of mutagenicity, ability to cross the blood?brain barrier, and powerful in vivo anti-glioblastoma activity. The overall attractive profile of 1 makes it an interesting compound for a bimodal therapeutic strategy against high grade gliomas.

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