Bimodal Therapeutic Agents Against Glioblastoma, One of the Most Lethal Forms of Cancer.

Couto, Marcos; Alamón, Catalina; Nievas, Susana; Perona, Marina; Dagrosa, María Alejandra; Teixidor, Francesc; Cabral, Pablo; Viñas, Clara; Cerecetto, Hugo

About 95 % of people diagnosed with glioblastoma die within five years. Glioblastoma is the most aggressive central nervous system tumour. It is necessary to make progress in the glioblastoma treatment so that advanced chemotherapy drugs or radiation therapy or, ideally, two‐in‐one hybrid systems should be implemented. Tyrosine kinase receptors–inhibitors and boron neutron capture therapy (BNCT), together, could provide a therapeutic strategy. In this work, sunitinib decorated‐carborane hybrids were prepared and biologically evaluated identifying excellent antitumoral‐ and BNCT‐agents. One of the selected hybrids was studied against glioma‐cells and found to be 4 times more cytotoxic than sunitinib and 1.7 times more effective than 10B‐boronophenylalanine fructose complex when the cells were irradiated with neutrons.

BORON-neutron capture therapy; GLIOBLASTOMA multiforme; DRUG therapy; CENTRAL nervous system; PEMETREXED

Chemistry - A European Journal, 2020, Vol 26, Issue 63, p14335

0947-6539

Academic Journal

10.1002/chem.202002963