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

Chemistry. 2020 Nov 11;26(63):14335-14340. doi: 10.1002/chem.202002963. Epub 2020 Oct 6.

Abstract

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.

Keywords: bimodal therapy; boron neutron capture therapy; carboranes; glioblastoma; sunitinib.

MeSH terms

  • Animals
  • Antineoplastic Agents* / pharmacology
  • Antineoplastic Agents* / therapeutic use
  • Boron Compounds
  • Boron Neutron Capture Therapy*
  • Brain Neoplasms* / drug therapy
  • Brain Neoplasms* / radiotherapy
  • Cell Line, Tumor
  • Cell Survival / drug effects*
  • Glioblastoma* / drug therapy
  • Glioblastoma* / radiotherapy
  • Humans
  • Mice
  • Pharmaceutical Preparations*
  • Phenylalanine

Substances

  • Antineoplastic Agents
  • Boron Compounds
  • Pharmaceutical Preparations
  • Phenylalanine