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

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 accumulate selectively tumour tissue still required. Hypoxia, deficiency oxygen tumor tissue, great challenge conventional treatment cancer, because hypoxic areas are resistant anticancer treatments. 2-Nitroimidazole derivatives known hypoxia markers due their enrichment by bioreduction cells. In present work, 2-nitroimidazole was chosen as starting point for synthesis boron-containing compound based on 1,3,5-triazine skeleton. Two o-carborane moieties were inserted achieve high ratio molecular weight, exploiting short PEG spacer enhance polarity and outdistance active part from core. The showed no toxicity normal human primary fibroblasts, while it noteworthy multiple myeloma cells together with consistent intracellular accumulation.