Triazinyl Architecture on Bifunctional Carboranyl Templates for the Production of Potential Neutron Capture Therapy Agents: Synthesis and Characterization of 1,3,5-Triazinylcarborane Derivatives

Abstract

A method for preparing triazinyl-substituted carboranyl systems using 1,2-, 1,7-, and 1,12-C₂B₁₀H₁₂ as cores and [di(alkyl)amino]triazine as substituents is described. A sulfur-containing o-carboranyl cage compound was also incorporated into the 1,3,5-triazine network to generate new types of hybrid compounds having a thio-ether linkage. Within the series of synthesized compounds, one showed increased water solubility arising from the effective camouflaging of the central p-carboranyl unit by the polar functional groups at the periphery. Furthermore, the same compound exhibited high boron uptake in B-16 melanoma cells with low toxicity, showing promise as a BNCT agent.

Key words

carborane scaffold - mono(triazinyl)carborane - bis(triazinyl)carborane - o-carboranylthiolate - triazine architecture - water-solubility - boron neutron capture therapy

References

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