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Boron Chemistry for Medical Applications: A Review of Recent Advances and Future Perspectives
Boron is a unique element that has many applications in various fields, including medicinal chemistry. Boron compounds have been recognized as potential agents for cancer treatment since several decades ago, but only a few have reached clinical trials or market approval. In this article, we review some of the recent advances and future perspectives of boron chemistry for medical applications, focusing on three main areas: boron neutron capture therapy (BNCT), boron-containing drugs, and boron-based imaging probes.
Boron Neutron Capture Therapy (BNCT)
BNCT is a form of radiotherapy that exploits the nuclear reaction between boron-10 and thermal neutrons, which produces high-energy alpha particles and lithium-7 nuclei that can selectively kill tumor cells. The key challenge of BNCT is to deliver sufficient amounts of boron-10 to the tumor site, while minimizing the toxicity to normal tissues. Various boron-containing compounds have been developed as BNCT agents, such as boronophenylalanine (BPA), sodium borocaptate (BSH), and boron clusters (e.g., carboranes, metallacarboranes, closo-dodecaborate). Some of these agents have been tested in clinical trials for brain tumors, head and neck cancers, melanoma, and other malignancies. However, the limited availability of neutron sources and the lack of effective delivery systems have hampered the widespread application of BNCT.
Boron can also be incorporated into small molecules or macromolecules as a pharmacophore or a bioisostere, conferring novel properties and functions to the resulting compounds. For example, bortezomib and ixazomib are boronic acid-based proteasome inhibitors that have been approved for the treatment of multiple myeloma and mantle cell lymphoma. Tavaborole is a boron-containing oxaborole that inhibits fungal protein synthesis and has been approved for the treatment of onychomycosis. Other examples of boron-containing drugs include anacardic acid derivatives for tuberculosis, benzoxaboroles for malaria and sleeping sickness, and boron dipyrromethene (BODIPY) derivatives for photodynamic therapy.
Boron-Based Imaging Probes
Boron can also be used as a contrast agent or a reporter for various imaging modalities, such as magnetic resonance imaging (MRI), positron emission tomography (PET), fluorescence imaging, and Raman spectroscopy. Boron-based imaging probes can provide information on the biodistribution, pharmacokinetics, metabolism, and target engagement of boron-containing drugs or BNCT agents. For example, fluorine-18-labeled BPA can be used as a PET tracer to monitor the uptake and retention of BPA in tumors prior to BNCT. BODIPY-based fluorescent probes can be used to visualize the intracellular localization and activation of boronic acid-based drugs. Boron-doped nanodiamonds can be used as MRI contrast agents or Raman reporters for multiplexed imaging.
Boron chemistry offers a rich and diverse platform for the development of novel and effective agents for cancer diagnosis and therapy. However, there are still many challenges and opportunities to overcome and explore in this field, such as improving the selectivity, stability, solubility, delivery, and safety of boron-containing compounds; designing multifunctional boron-based systems that can integrate imaging and therapy; and discovering new biological targets and mechanisms of action for boron-based interventions. We hope that this article will stimulate further research and innovation in boron chemistry for medical applications. a474f39169