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

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 sh...

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Bibliographic Details
Published in:Chemistry : a European journal 2020-11, Vol.26 (63), p.14335-14340
Main Authors: Couto, Marcos, Alamón, Catalina, Nievas, Susana, Perona, Marina, Dagrosa, María Alejandra, Teixidor, Francesc, Cabral, Pablo, Viñas, Clara, Cerecetto, Hugo
Format: Article
Language:English
Subjects:
Animals
Anticancer properties
Antineoplastic Agents - pharmacology
Antineoplastic Agents - therapeutic use
bimodal therapy
Boron
Boron Compounds
Boron Neutron Capture Therapy
Brain cancer
Brain Neoplasms - drug therapy
Brain Neoplasms - radiotherapy
Carborane
carboranes
Cell Line, Tumor
Cell Survival - drug effects
Central nervous system
Chemical compounds
Chemistry
Chemotherapy
Cytotoxicity
Glioblastoma
Glioblastoma - drug therapy
Glioblastoma - radiotherapy
Glioma cells
Humans
Hybrid systems
Hybrids
Kinases
Mice
Neutrons
Nuclear capture
Pharmaceutical Preparations
Pharmacology
Phenylalanine
Protein-tyrosine kinase
Radiation
Radiation therapy
sunitinib
Targeted cancer therapy
Tumors
Tyrosine
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Summary: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. Compounds for bimodal cancer‐treatment, based on tyrosine kinase receptors–inhibitors and boron neutron capture therapy (BNCT), were successfully developed. The single molecules, sunitinib decorated‐carborane hybrids, could represent a significant advance in cancer treatment (see figure).
ISSN:0947-6539
1521-3765
DOI:10.1002/chem.202002963