Comparison of Radionuclide Drug Conjugates With Boron Neutron Capture Therapy: An Overview of Targeted Charged Particle Radiation Therapy.

Targeted charged alpha- and beta-particle therapies are currently being used in clinical radiation treatments as newly developed methods for either killing or controlling tumor cell growth. The alpha particles can be generated either through a nuclear decay reaction or in situ by a nuclear fission reaction such as the boron neutron capture reaction. Different strategies have been employed to improve the selectivity and delivery of radiation dose to tumor cells based on the source of the clinically used alpha particles.

In silico assessments of the small molecular boron agents to pave the way for artificial intelligence-based boron neutron capture therapy.

Boron neutron capture therapy (BNCT) is a highly targeted, selective and effective technique to cure various types of cancers, with less harm to the healthy cells. In principle, BNCT treatment needs to distribute the boron (B) atoms inside the tumor tissues, selectively and homogeneously, as well as to initiate a nuclear fission reaction by capturing sufficient neutrons which releases high linear energy particles to kill the tumor cells. In BNCT, it is crucial to have high quality boron agents with acceptable bio-selectivity, homogeneous distribution and deliver in required quantity, similar to chemotherapy and other radiotherapy for tumor treatment.

Nanostructured boron agents for boron neutron capture therapy: a review of recent patents.

Boron neutron capture therapy (BNCT) is a potential radiation therapy modality for cancer, and tumor-targeted stable boron-10 (B) delivery agents are an important component of BNCT. Currently, two low-molecular-weight boron-containing compounds, sodium mercaptoundecahydro--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.

Next generation of boron neutron capture therapy (BNCT) agents for cancer treatment.

Boron neutron capture therapy (BNCT) is one of the most promising treatments among neutron capture therapies due to its long-term clinical application and unequivocally obtained success during clinical trials. Boron drug and neutron play an equivalent crucial role in BNCT. Nevertheless, current clinically used l-boronophenylalanine (BPA) and sodium borocaptate (BSH) suffer from large uptake dose and low blood to tumor selectivity, and that initiated overwhelm screening of next generation of BNCT agents.

Functionalized Boron Nanoparticles as Potential Promising Antimalarial Agents.

Boron nanoparticles (BNPs), functionalized with hydroxyl groups, were synthesized by a cascade process, followed by bromination and hydrolyzation reactions. These functionalized BNPs, (B (OH) ), were characterized using H and B NMR spectra, Fourier-transform infrared (FT-IR) spectroscopy, inductively coupled plasma-optical emission spectroscopy (ICP-OES), transmission electron microscopy (TEM), dynamic light scattering (DLS), and X-ray photoelectron spectroscopy (XPS) methods. These nanoparticles were also evaluated for their antimalarial activity against (3D7 strain) with an IC value of 0.

Carboxyboranylamino ethanol: unprecedented discovery of boron agents for neutron capture therapy in cancer treatment.

Carboxyboranylamino ethanol (MeN(BHCOH)CHCHOH, 1) was prepared in 75.0% yield by an amine-exchange reaction. Compound 1 shows lower cytotoxicity and higher anti-tumor efficacy towards the SCCVII cell line in comparison with 4-borono-L-phenylalanine (BPA) and methyl 2-hydroxyl-5-(1'--carbonylmethyl-1',2',3'-triazol-4'-yl)-benzonate (2).

Organoboron Compounds: Effective Antibacterial and Antiparasitic Agents.

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.

Synthesis, Molecular Docking, and In Vitro Boron Neutron Capture Therapy Assay of Carboranyl Sinomenine.

In comparison with pristine sinomenine and carborane precursors, the calculations of molecular docking with matrix metalloproteinases (MMPs) and methylcarboranyl--butyl sinomenine showed improved interactions. Accordingly, methylcarboranyl--butyl sinomenine shows a high potential in the treatment of rheumatoid arthritis (RA) in the presence of slow neutrons. The reaction of potassium salt of sinomenie, which is generated from the deprotonation of sinomenine () using potassium carbonate in a solvent of ,-dimethyl formamide, with 4-methylcarboranyl--butyl iodide, () forms methylcarboranyl--butyl sinomenine () in 54.

Boron Chemistry for Medical Applications.

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.

Synthesis and in vitro anti-tumor activity of carboranyl levodopa.

Reactions of closo-1-Me-2-Iodobutyl-1,2-closo-dicarborane, 1-Me-2-I(CH)-CBH, with l-dopa methyl ester can produce carboranyl l-dopa methyl esters in 54% yield in the presence of sodium hydroxide. The appended closo-carboranes can be decapitated with sodium hydroxide in a mixed solvent of ethanol and deionized water to produce highly water-soluble carboranyl levodopa in 64% yield. All the new compounds were characterized by H, C, B NMR, FT-IR spectroscopy and elemental analysis.

Liquid-Phase Synthesis of Boron Isocyanates: Precursors to Boron Nanoparticles.

The practical application of boron isocyanates has been hindered by their extremely high sensitivity and reactivity toward air and moisture. A convenient synthetic method in a suitable liquid media is reported for practical utilization of boron isocyanates. According to NMR studies, the in situ generated boron isocyanates can be stored for at least one month under an inert atmosphere at -20 °C without noticeable decomposition.

The Current Status and Perspectives of Delivery Strategy for Boronbased Drugs.

Boron-containing compounds are essential micronutrients for animals and plants despite their low-level natural occurrence. They can strengthen the cell walls of the plants and they play important role in supporting bone health. However, surprisingly, boron-containing compounds are seldom found in pharmaceutical drugs.

Advanced Developments in Cyclic Polymers: Synthesis, Applications, and Perspectives.

Due to the topological effect, cyclic polymers demonstrate different and unique physical and biological properties in comparison with linear counterparts having the same molecular-weight range. With advanced synthetic and analytic technologies, cyclic polymers with different topologies, e.g.

Cross-coupling reaction between arylboronic acids and carboranyl iodides catalyzed by graphene oxide (GO)-supported Pd(0) recyclable nanoparticles for the synthesis of carboranylaryl ketones.

Well-dispersed palladium(0) nanoparticles with small and narrow size distributions were synthesized conveniently on a graphene oxide (GO) surface. The GO-supported nano-Pd(0) was found to be a highly efficient and recyclable catalyst for the carbonylative cross-coupling reaction between arylboronic acids and aryl and carboranyl iodides, respectively. Benzophenone and a series of carboranylaryl ketones, 1-R-2-[C(=O)Ar]-1,2-C2B10H10 (R = H, Me, Ph; Ar = C6H5, C6H4-4-OMe and C6H4-4-F), were synthesized and fully characterized.

Applications and perspectives of boron-enriched nanocomposites in cancer therapy.

Recently, boron compounds have attracted increasing attention both in academic laboratories and in the pharmaceutical industry. Boron, in particular the (10)B isotope, has the unique capability of absorbing a slow neutron to initiate a nuclear reaction with release of energetic particles such as α- and Li-particles, which is not observed in its carbon analogues. The nuclear capture reaction concept has been adopted in radiation therapy and used in boron neutron capture therapy (BNCT).

Atmospheric pressure aminocarbonylation of aryl iodides using palladium nanoparticles supported on MOF-5.

An efficient amide synthesis by atmospheric pressure aminocarbonylation using palladium nanoparticles supported on MOF-5 is reported. Interestingly, only 0.5 wt% palladium loading was required to achieve high yields.

Stabilized well-dispersed Pd(0) nanoparticles for aminocarbonylation of aryl halides.

Well-dispersed palladium (0) nanoparticles stabilized with phosphonium based ionic liquid were synthesized conveniently and fully characterized. A catalyst system comprising of the Pd(0) nanoparticles and a base was found to be recyclable and efficient for the aminocarbonylation reaction of aryl iodide in ionic liquid media. In the presence of potassium tert-butyloxide, for the relatively stable aryl chloride and bromide substrates, medium activities were achieved for the catalyst.

Application of cycloaddition reactions to the syntheses of novel boron compounds.

This review covers the application of cycloaddition reactions in forming the boron-containing compounds such as symmetric star-shaped boron-enriched dendritic molecules, nano-structured boron materials and aromatic boronic esters. The resulting boron compounds are potentially important reagents for both materials science and medical applications such as in boron neutron capture therapy (BNCT) in cancer treatment and as drug delivery agents and synthetic intermediates for carbon-carbon cross-coupling reactions. In addition, the use of boron cage compounds in a number of cycloaddition reactions to synthesize unique aromatic species will be reviewed briefly.

Catalytic phenylborylation reaction by iridium(0) nanoparticles produced from hydridoiridium carborane.

Well-dispersed iridium(0) nanoparticles stabilized with the ionic liquid, trihexyltetradecylphosphonium methylsulfonate, [THTdP][MS], have been successfully prepared by reduction of the precursor hydridoiridium carborane, (Ph 3P) 2Ir(H)(7,8- nido-C 2B 9H 11). The iridium nanoparticles were found to be active catalysts for arylborylation, forming boric acids. The activity of the catalyst has been investigated as a function of the activating base, and reaction conditions.

Latest developments in the catalytic application of nanoscaled neutral group 8-10 metals.

In the last few decades, the synthesis and catalytic application of nanoscaled particles prepared from Group 8-10 (formerly Group VIIIB) elements have been widely explored and have achieved promising results. The innovative use of these nanoparticle catalysts may provide new opportunities in the efficient combination of conventionally used homogenous and heterogeneous catalysts. Conventional homogeneous catalysts pose extraction and recycling difficulties when dealing with metal complexes and/or ligands, whereas heterogeneous catalysts generally require more pressing experimental conditions, such as high temperatures and high pressures, to be effective.

Ruthenium(0) nanoparticle-catalyzed isotope exchange between 10B and 11B nuclei in decaborane(14).

Well dispersed ruthenium(0) nanoparticles, stabilized in the ionic liquid agent, trihexyltetradecylphosphonium dodecylbenzenesulfonate, have been successfully prepared via a reduction reaction of the precursor [CpRuCp*RuCp*]PF6 (Cp* = C5Me5). The ruthenium(0) nanoparticles were shown to catalyze the isotope exchange reaction between 10B enriched diborane and natural abundant B10H14 to produce highly 10B enriched (approximately 90%) decaborane(14) products. The ruthenium(0) nanoparticles were characterized by TEM, XRD, and XPS.

Substituted carborane-appended water-soluble single-wall carbon nanotubes: new approach to boron neutron capture therapy drug delivery.

Substituted C(2)B(10) carborane cages have been successfully attached to the side walls of single-wall carbon nanotubes (SWCNTs) via nitrene cycloaddition. The decapitations of these C(2)B(10) carborane cages, with the appended SWCNTs intact, were accomplished by the reaction with sodium hydroxide in refluxing ethanol. During base reflux, the three-membered ring formed by the nitrene and SWCNT was opened to produce water-soluble SWCNTs in which the side walls are functionalized by both substituted nido-C(2)B(9) carborane units and ethoxide moieties.