Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 26, Issue 63, Pages 14335-14340Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.202002963
Keywords
bimodal therapy; boron neutron capture therapy; carboranes; glioblastoma; sunitinib
Categories
Funding
- FCE-ANII [FCE_3_2018_1_148288]
- CSIC-Universidad de la Republica (UdelaR) (Grupo I+D) [CSIC-421]
- ANII [POS_NAC_2015_1_110068]
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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(10)B-boronophenylalanine fructose complex when the cells were irradiated with neutrons.
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