Boron compounds now have many applications in a number of fields, including Medicinal Chemistry. Although the uses of boron compounds in pharmacological science have been recognized several decades ago, surprisingly few are found in pharmaceutical drugs. The boron-containing compounds epitomize a new class for medicinal chemists to use in their drug designs. Carboranes are a class of organometallic compounds containing carbon (C), boron (B), and hydrogen (H) and are the most widely studied boron compounds in medicinal chemistry. Additionally, other boron-based compounds are of great interest, such as dodecaborate anions, metallacarboranes and metallaboranes. The boron neutron capture therapy (BNCT) has been utilized for cancer treatment from last decade, where chemotherapy and radiation have their own shortcomings. However, the improvement in the already existing (BPA and/or BSH) localized delivery agents or new tumor-targeted compounds are required before realizing the full clinical potential of BNCT. The work outlined in this short review addresses the advancements in boron containing compounds. Here, we have focused on the possible clinical implications of the new and improved boron-based biologically active compounds for BNCT that are reported to have in vivo and/or in vitro efficacy.

The unique electron deficiency and coordination property of boron led to a wide range of applications in chemistry, energy research, materials science and the life sciences. The use of boron-containing compounds as pharmaceutical agents has a long history, and recent developments have produced encouraging strides. Boron agents have been used for both radiotherapy and chemotherapy. In radiotherapy, boron neutron capture therapy (BNCT) has been investigated to treat various types of tumors, such as glioblastoma multiforme (GBM) of brain, head and neck tumors, etc. Boron agents playing essential roles in such treatments and other well-established areas have been discussed elsewhere. Organoboron compounds used to treat various diseases besides tumor treatments through BNCT technology have also marked an important milestone. Following the clinical introduction of bortezomib as an anti-cancer agent, benzoxaborole drugs, tavaborole and crisaborole, have been approved for clinical use in the treatments of onychomycosis and atopic dermatitis. Some heterocyclic organoboron compounds represent potentially promising candidates for anti-infective drugs. This review highlights the clinical applications and perspectives of organoboron compounds with the natural boron atoms in disease treatments without neutron irradiation. The main topic focuses on the therapeutic applications of organoboron compounds in the diseases of tuberculosis and antifungal activity, malaria, neglected tropical diseases and cryptosporidiosis and toxoplasmosis.

Nanostructured boron compounds have emerged as one of the promising frontiers in boron chemistry. These species possess unique physical and chemical properties in comparison with classical small boron compounds. The nanostructured boron composites generally have large amounts of boron contents and thus have the potential to deliver significant amount of boron to the tumor cells, that is crucial for boron neutron capture therapy (BNCT). In theory, BNCT is based on a nuclear capture reaction with the ¹⁰B isotope absorbing a slow neutron to initiate a nuclear fission reaction with the release of energetic particles, such as lithium and helium (α particles), which travel the distance of around nine microns within the cell DNA or RNA to destroy it. The recent studies have demonstrated that the nanostructured boron composites can be combined with the advanced targeted drug delivery system and drug detection technology. The successful combination of these three areas should significantly improve the BNCT in cancer treatment. This mini review summarizes the latest developments in this unique area of cancer therapy.

Boron neutron capture therapy (BNCT) is a potential radiation therapy modality for cancer, and tumor-targeted stable boron-10 (¹⁰B) delivery agents are an important component of BNCT. Currently, two low-molecular-weight boron-containing compounds, sodium mercaptoundecahydro-closo-dodecaborate (BSH) and boronophenylalanine (BPA), are mainly used in BNCT. Although both have suboptimal tumor selectivity, they have shown some therapeutic benefit in patients with high-grade glioma and several other tumors. To improve the efficacy of BNCT, great efforts have been devoted for the development of new boron delivery agents with better uptake and favorable pharmacokinetic profiles. This article reviews the application and research progress of boron nanomaterials as boron carriers in boron neutron capture therapy and hopes to stimulate people’s interest in nanomaterial-based delivery agents by summarizing various kinds of boron nanomaterial patents disclosed in the past decade.