4.5 Article

Synthesis and Characterisation of a Boron-Rich Symmetric Triazine Bearing a Hypoxia-Targeting Nitroimidazole Moiety

Journal

SYMMETRY-BASEL
Volume 13, Issue 2, Pages -

Publisher

MDPI
DOI: 10.3390/sym13020202

Keywords

BNCT; triazines; carboranes; nitroimidazole; boron accumulation

Funding

  1. Progetto Ricerca Locale-Universita del Piemonte Orientale (DSF) 2019
  2. Paula C. and Rodger O. Riney Blood Cancer Research Initiative Fund
  3. United States National Institutes of Health (NIH) [U54CA199092]

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Boron Neutron Capture Therapy (BNCT) shows promise in treating non-curable cancers, with a new boron compound being discovered to selectively accumulate in tumor tissue. Hypoxia poses a challenge in cancer treatment, but a new compound exhibits toxicity in multiple myeloma cells and consistent intracellular boron accumulation.
Boron Neutron Capture Therapy (BNCT) is a binary therapy that promises to be suitable in treating many non-curable cancers. To that, the discovery of new boron compounds able to accumulate selectively in the tumour tissue is still required. Hypoxia, a deficiency of oxygen in tumor tissue, is a great challenge in the conventional treatment of cancer, because hypoxic areas are resistant to conventional anticancer treatments. 2-Nitroimidazole derivatives are known to be hypoxia markers due to their enrichment by bioreduction in hypoxic cells. In the present work, 2-nitroimidazole was chosen as the starting point for the synthesis of a new boron-containing compound based on a 1,3,5-triazine skeleton. Two o-carborane moieties were inserted to achieve a high ratio of boron on the molecular weight, exploiting a short PEG spacer to enhance the polarity of the compound and outdistance the active part from the core. The compound showed no toxicity on normal human primary fibroblasts, while it showed noteworthy toxicity in multiple myeloma cells together with a consistent intracellular boron accumulation.

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