Synthesis of 1-Amino-3-{2-[7-(6-deoxy-α/β-D-galactopyranos-6-yl)-1,7-dicarba-closo-dodecaboran(12)-1-yl]ethyl}cyclobutanecarboxylic Acid Hydrochloride

2002 ◽  
Vol 67 (6) ◽  
pp. 836-842 ◽  
Author(s):  
George W. Kabalka ◽  
Bhaskar C. Das ◽  
Sasmita Das ◽  
Guishing Li ◽  
Rajiv Srivastava ◽  
...  
Keyword(s):  
Amino Acid ◽  
Cancer Cells ◽  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Neutron Capture Therapy ◽  
Toxicity Data ◽  
Boron Neutron Capture ◽  
Cyclobutanecarboxylic Acid ◽  
Strecker Synthesis ◽  
Acid Hydrochloride

1-Amino-3-{2-[7-(6-deoxy-α/β-D-galactopyranos-6-yl)-1,7-dicarba-closo-dodecaboran(12)-1-yl]ethyl}cyclobutanecarboxylic acid was synthesized as a potential new agent for boron neutron capture therapy. The key step in the synthesis is the alkylation of 3-{2-[1,7-dicarba-closo-dodecaboran(12)-1-yl]ethyl}cyclobutanone ethylene monothioketal with 1,2:3,4-di-O-isopropylidene-6-O-triflyl-α-D-galactopyranose which gave the precursor ketone that was then converted to the title amino acid via a Bücherer-Strecker synthesis followed by removal of isopropylidene groups in HCl. Preliminary toxicity data in A 435 cancer cells were obtained.

Bahan Sasaran Sebagai Sumber Neutron yang Optimal untuk Boron Neutron Capture Therapy (BNCT)

2017 ◽  
Vol 1 ◽  
pp. 104
Author(s):  
Yan Surono ◽  
C Cari ◽  
Yohannes Sarjono
Keyword(s):  
Cancer Cells ◽  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Neutron Capture Therapy ◽  
Radioactive Elements ◽  
Therapeutic Technique ◽  
The Core ◽  
Boron Neutron Capture ◽  
Deadly Disease ◽  
Α Particles

<p><strong>Abstract</strong> Cancer is a deadly disease that exist on planet earth. Efforts were made to be able to kill cancer cells either by manual operation or by radiotherapy. One way to use energy radiation radioactive elements as killers of cancer cells is Boron Neutron Capture Therapy (BNCT). BNCT is a therapeutic technique that utilizes the interaction of neutron capture by the core 10B will produce α-particles and nuclei 7Li results by reaction 10B (n, α) 7Li. It therefore requires a material that will produce neutrons used in BNCT. Materials  target that will be searched in order to obtain optimal materials according to the requirements provided by the International Atomic Agency (IAEA).<em></em></p><p><em> </em></p><p><strong>Keywords </strong>: Kanker, Material, Neutron, BNCT</p><p align="center"><strong><em> </em></strong></p><p><strong>Abstrak</strong> Kanker adalah salah satu penyakit yang mematikan yang ada di planet bumi. Upaya upaya dilakukan untuk dapat membunuh sel kanker baik itu  secara operasi manual maupun dengan cara radioterapi. Salah satu cara yang memanfaatkan energi radiasi unsur unsur radioaktif sebagai pembunuh sel kanker adalah Boron Neutron Capture Therapy (BNCT). BNCT merupakan teknik terapi yang memanfaatkan interaksi tangkapan neutron oleh inti 10B yang akan menghasilkan partikel-α dan inti hasil 7Li melalui reaksi 10B(n,α) 7Li. Oleh sebab itu diperlukan material yang akan menghasilkan neutron digunakan dalam BNCT. Bahan - bahan sasaran yang akan ditelusur dalam upaya mendapatkan bahan yang optimal sesuai persyaratan yang diberikan oleh International Atomic Agency (IAEA).</p><p><em> </em></p><p><strong>Kata Kunci </strong>: Kanker, Material, Neutron, BNCT</p>

scholarly journals Cyclic-RGDyC functionalized liposomes for dual-targeting of tumor vasculature and cancer cells in glioblastoma: An in vitro boron neutron capture therapy study

Oncotarget ◽  
2017 ◽  
Vol 8 (22) ◽  
pp. 36614-36627 ◽  
Author(s):  
Weirong Kang ◽  
Darren Svirskis ◽  
Vijayalekshmi Sarojini ◽  
Ailsa L. McGregor ◽  
Joseph Bevitt ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Tumor Vasculature ◽  
Neutron Capture Therapy ◽  
Boron Neutron Capture ◽  
Dual Targeting

scholarly journals In Vitro Studies to Define the Cell-Surface and Intracellular Targets of Polyarginine-Conjugated Sodium Borocaptate as a Potential Delivery Agent for Boron Neutron Capture Therapy

Cells ◽  
2020 ◽  
Vol 9 (10) ◽  
pp. 2149
Author(s):  
Atsushi Fujimura ◽  
Seiji Yasui ◽  
Kazuyo Igawa ◽  
Ai Ueda ◽  
Kaori Watanabe ◽  
...  
Keyword(s):  
Amino Acid ◽  
Cell Surface ◽  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Cell Membrane Permeability ◽  
Neutron Capture Therapy ◽  
Translational Machinery ◽  
Boron Neutron Capture ◽  
The Future ◽  
Intracellular Targets

Boron neutron capture therapy (BNCT) requires pharmaceutical innovations and molecular-based evidence of effectiveness to become a standard cancer therapeutic in the future. Recently, in Japan, 4-borono-L-phenylalanine (BPA) was approved as a boron agent for BNCT against head and neck (H&N) cancers. H&N cancer appears to be a suitable target for BPA-BNCT, because the expression levels of L-type amino acid transporter 1 (LAT1), one of the amino acid transporters responsible for BPA uptake, are elevated in most cases of H&N cancer. However, in other types of cancer including malignant brain tumors, LAT1 is not always highly expressed. To expand the possibility of BNCT for these cases, we previously developed poly-arginine peptide (polyR)-conjugated mercaptoundecahydrododecaborate (BSH). PolyR confers the cell membrane permeability and tumor selectivity of BSH. However, the molecular determinants for the properties are not fully understood. In this present study, we have identified the cluster of differentiation 44 (CD44) protein and translational machinery proteins as a major cell surface target and intracellular targets of BSH-polyR, respectively. CD44, also known as a stem cell-associated maker in various types of cancer, is required for the cellular uptake of polyR-conjugated molecules. We showed that BSH-polyR was predominantly delivered to a CD44High cell population of cancer cells. Once delivered, BSH-polyR interacted with the translational machinery components, including the initiation factors, termination factors, and poly(A)-biding protein (PABP). As a proof of principle, we performed BSH-polyR-based BNCT against glioma stem-like cells and revealed that BSH-polyR successfully induced BNCT-dependent cell death specifically in CD44High cells. Bioinformatics analysis indicated that BSH-polyR would be suitable for certain types of malignant tumors. Our results shed light on the biochemical properties of BSH-polyR, which may further contribute to the therapeutic optimization of BSH-BNCT in the future.

Cellular uptake evaluation of pentagamaboronon-0 (PGB-0) for boron neutron capture therapy (BNCT) against breast cancer cells

2019 ◽  
Vol 37 (6) ◽  
pp. 1292-1299
Author(s):  
Adam Hermawan ◽  
Ratna Asmah Susidarti ◽  
Ratna Dwi Ramadani ◽  
Lailatul Qodria ◽  
Rohmad Yudi Utomo ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Cellular Uptake ◽  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Breast Cancer Cells ◽  
Neutron Capture Therapy ◽  
Boron Neutron Capture

scholarly journals Analysis of Radiation Interactions and Biological Effects for Boron Neutron Capture Therapy

2018 ◽  
Vol 35 (3) ◽  
pp. 203-207
Author(s):  
Ren-Tai Chiang
Keyword(s):  
Cell Death ◽  
Cancer Cells ◽  
Blood Supply ◽  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Biological Effects ◽  
Neutron Capture Therapy ◽  
Boron Neutron Capture ◽  
Cancer Tumor ◽  
Ionizing Radiations

 The direct and indirect ionizing radiation sources for boron neutron capture therapy (BNCT)are identi?ed. The mechanisms of physical, chemical and biological radiation interactions for BNCT are systematically described and analyzed. The relationship between the effect of biological radiation and radiation dose are illustrated and analyzed for BNCT. If the DNAs in chromosomes are damaged by ion- izing radiations, the instructions that control the cell function and reproduction are also damaged. This radiation damage may be reparable, irreparable, or incorrectly repaired. The irreparable damage can result in cell death at next mitosis while incorrectly repaired damage can result in mutation. Cell death leads to variable degrees of tissue dysfunction, which can affect the whole organism’s functions. Can- cer cells cannot live without oxygen and nutrients via the blood supply. A cancer tumor can be shrunk by damaging angiogenic factors and/or capillaries via ionizing radiations to decrease blood supply into the cancer tumor. The collisions between ionizing radiations and the target nuclei and the absorption of the ultraviolet, visible light, infrared and microwaves from bremsstrahlung in the tumor can heat up and damage cancer cells and function as thermotherapy. The cancer cells are more chemically and biologically sensitive at the BNCT-induced higher temperatures since free-radical-induced chemical re- actions are more random and vigorous at higher temperatures after irradiation, and consequently the cancer cells are harder to divide or even survive due to more cell DNA damage. BNCT is demonstrated via a recent clinical trial that it is quite effective in treating recurrent nasopharyngeal cancer.

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