Abstract
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.
Highlights
Boron Neutron Capture Therapy is a binary treatment in which boron compounds are introduced into cancer cells and irradiated by thermal neutrons
As stated in the introduction, we have previously reported a hypoxia-targeted Boron Neutron Capture Therapy (BNCT) agent B381, based on 2-nitroimidazole, which has shown specific accumulation in cancer tissues in vitro and in vivo due to the specific reduction of the 2-nitroimidazole and con
Because B381 compound included only one boron atom in each molecule, it resulted in relatively low boron tissue accumulation
Summary
Boron Neutron Capture Therapy is a binary treatment in which boron compounds are introduced into cancer cells and irradiated by thermal neutrons. The tumor-targeting ability and the selectivity are among the most important requisites for new compounds They should be able to accumulate the commonly accepted optimal boron amount for neutron capture therapy, namely ≥109 10B atoms per cell, corresponding to 20 μg boron per g of tumour tissue [3]. 2-Nitroimidazole is known to undergo bioreductive trapping in hypoxic cells, making it a promising starting point for the design of hypoxia-targeting agents [5]. Its ability to accumulate in hypoxic cells by bioreductive trapping makes 2-nitroimidazole a promising starting point for the design of hypoxia-targeting agents. A symmetrical hybrid compound containing two carborane residues and 2-nitroimidazole moiety on a triazine scaffold is described as a potential agent for BNCT
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