4.6 Review

Organoboronic acids/esters as effective drug and prodrug candidates in cancer treatments: challenge and hope

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Borax regulates iron chaperone- and autophagy-mediated ferroptosis pathway in glioblastoma cells

Ceyhan Hacioglu et al.

Summary: In this study, the effects of borax on the ferroptosis signaling pathway in GBM cells were investigated. Borax significantly reduced cell viability and altered cell proliferation and cycle in GBM cells. It induced apoptosis by downregulating PCBP1, GSH, and GPx4 expressions and upregulating Beclin1, MDA, and ACSL4 expressions. These findings suggest that borax has potential as an anticancer treatment for GBM by regulating the PCBP1/Beclin1/GPx4/ACSL4 signaling pathways.

ENVIRONMENTAL TOXICOLOGY (2023)

Article Chemistry, Medicinal

Design and discovery of novel dipeptide boronic acid ester proteasome inhibitors, an oral slowly-released prodrug for the treatment of multiple myeloma

Xueyuan Wang et al.

Summary: This study designed, synthesized, and biologically investigated a series of dipeptide boronic acid esters as novel oral proteasome inhibitors targeting the beta 5 subunit of 20S proteasome in multiple myeloma. Some compounds showed potent antiproliferative activity against RPMI-8226 cell line, and compound 18u exhibited good stability and hydrolysis rate in simulated gastric juice and simulated intestinal juice. Moreover, compound 18u displayed strong in vivo anticancer efficacy in a human MM xenograft mouse model.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2023)

Article Biochemistry & Molecular Biology

Calcium fructoborate regulate colon cancer (Caco-2) cytotoxicity through modulation of apoptosis

Mehmet A. Kisacam et al.

Summary: This study found that calcium fructoborate (CaFB) has anti-proliferative effects on colon cancer cells, potentially by inducing apoptosis and activating autophagy.

JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY (2022)

Article Biochemistry & Molecular Biology

Boric acid suppresses cell proliferation by TNF signaling pathway mediated apoptosis in SW-480 human colon cancer line

Murat Sevimli et al.

Summary: The study found that boric acid inhibited cell proliferation and induced apoptosis in the human colon adenocarcinoma cell line SW-480, in both 2D and 3D culture conditions. Additionally, qRT-PCR analysis revealed that the observed apoptotic process was associated with the TNF signaling pathway. Boric acid may be considered a potential anti-cancer agent candidate for colon cancer treatment.

JOURNAL OF TRACE ELEMENTS IN MEDICINE AND BIOLOGY (2022)

Review Pharmacology & Pharmacy

Boronic Acid as a Promising Class of Chemical Entity for Development of Clinical Medicine for Targeted Therapy of Cancer

Takumi Watanabe et al.

Summary: Bortezomib, the first medicine containing the boron element, has the ability to form reversible covalent bonds with hydroxy groups commonly found in catalytic sites of proteolytic enzymes. Boronic acid is now considered an important molecule in medicinal chemistry toolbox due to the success of bortezomib and its use in designing protease inhibitors. This review article provides an overview of the development of bortezomib and highlights the construction of potent analogs of tyropeptin A, a natural proteasome inhibitor, using boronic acid. It also showcases representative stereoselective synthetic methods of alpha-aminoboronic acid.

YAKUGAKU ZASSHI-JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN (2022)

Article Biochemistry & Molecular Biology

Brain Boron Level, DNA Content, and Myeloperoxidase Activity of Metformin-Treated Rats in Diabetes and Prostate Cancer Model

Armagan Begum Ozel et al.

Summary: This study investigated the effect of metformin on brain boron levels and oxidative brain damage in rats with diabetes and prostate cancer. The findings suggest that metformin may protect against brain damage by increasing boron levels.

BIOLOGICAL TRACE ELEMENT RESEARCH (2022)

Review Biochemistry & Molecular Biology

Natural source, bioactivity and synthesis of 3-Arylcoumarin derivatives

Qiang Zhang et al.

Summary: 3-arylcoumarins with different pharmacological properties are widely found in natural plants. Extensive research on these compounds is due to their therapeutic effects and ease of isolation. Therefore, 3-arylcoumarins can be considered useful structures for designing novel compounds with potential pharmacological interest.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2022)

Article Biochemistry & Molecular Biology

Anti-cancer effect of boron derivatives on small-cell lung cancer

Emre Cebeci et al.

Summary: The study demonstrated the anti-cancer activity of boric acid, sodium pentaborate pentahydrate, and sodium perborate tetrahydrate against small-cell lung cancer cells. The mechanisms involved apoptosis and cell cycle arrest.

JOURNAL OF TRACE ELEMENTS IN MEDICINE AND BIOLOGY (2022)

Review Biochemistry & Molecular Biology

Inhibitors of glucosamine-6-phosphate synthase as potential antimicrobials or antidiabetics - synthesis and properties

Joanna Stefaniak et al.

Summary: Glucosamine-6-phosphate synthase (GlcN-6-P synthase) is an important target for the development of antimicrobial agents and antidiabetic drugs. Various compounds have been identified as inhibitors of this enzyme, but their antimicrobial activity is relatively low and they have poor penetration ability. The pro-drug approach has been used to improve the antimicrobial activity of these inhibitors. Additionally, heterocyclic and polycyclic compounds have shown antimicrobial activity and potential as inhibitors of the enzyme, pending confirmation of their selective toxicity.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2022)

Article Chemistry, Analytical

3-Thienylboronic Acid as a Receptor for Diol-Containing Compounds: A Study by Isothermal Titration Calorimetry

Yulia Efremenko et al.

Summary: The electrochemical activity of 3-thienylboronic acid makes it a promising receptor material for sensor applications. The highest binding enthalpy was observed for sorbitol and fructose, with a significant increase in binding enthalpy and constant with pH change.

CHEMOSENSORS (2022)

Article Chemistry, Inorganic & Nuclear

In Vivo Assessment of the Effect of Hexagonal Boron Nitride Nanoparticles on Biochemical, Histopathological, Oxidant and Antioxidant Status

Fatih Kar et al.

Summary: The study found that low doses of hBN NPs may not be toxic in biomedical applications, while high doses can cause significant damage to multiple organs in rats. This suggests that the toxicity of hBN NPs depends on the dose, with different doses exhibiting different biological system effects.

JOURNAL OF CLUSTER SCIENCE (2021)

Article Chemistry, Medicinal

Computational Bioactivity Analysis and Bioisosteric Investigation of the Approved Breast Cancer Drugs Proposed New Design Drug Compounds: Increased Bioactivity Coming with Silicon and Boron

Esma Eryilmaz Dogan

Summary: This study aimed to design in silico drug candidates possessing multi-targeted bioactivity for combating multidrug resistance in breast cancer. Through molecular modeling and bioisosteric modifications, promising new molecules with enhanced bioactivity effects were identified, particularly with the incorporation of boron and silicon.

LETTERS IN DRUG DESIGN & DISCOVERY (2021)

Article Oncology

Global cancer statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries

Hyuna Sung et al.

Summary: The global cancer burden in 2020 saw an estimated 19.3 million new cancer cases and almost 10.0 million cancer deaths. Female breast cancer surpassed lung cancer as the most commonly diagnosed cancer, while lung cancer remained the leading cause of cancer death. These trends are expected to rise in 2040, with transitioning countries experiencing a larger increase compared to transitioned countries due to demographic changes and risk factors associated with globalization and a growing economy. Efforts to improve cancer prevention measures and provision of cancer care in transitioning countries will be crucial for global cancer control.

CA-A CANCER JOURNAL FOR CLINICIANS (2021)

Review Oncology

Boron Neutron Capture Therapy: A Review of Clinical Applications

Timothy D. Malouff et al.

Summary: Boron neutron capture therapy (BNCT) is an emerging treatment modality that utilizes boron-10 to target tumors and has shown promising results in various cancer types in clinical studies.

FRONTIERS IN ONCOLOGY (2021)

Article Medicine, Research & Experimental

The Use of In Silico Tools for the Toxicity Prediction of Potential Inhibitors of SARS-CoV-2

Varsha Bhat et al.

Summary: The study utilized various computational tools to predict the toxicity of 19 experimental compounds, revealing encouraging toxicity profiles for most compounds, which can assist in further drug development efforts to combat Covid-19.

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Reactive Oxygen Species (ROS)-Sensitive Prodrugs of the Tyrosine Kinase Inhibitor Crizotinib

Bjoern Bielec et al.

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Self-assembly of oxidation-responsive polyethylene glycol-paclitaxel prodrug for cancer chemotherapy

Chengyuan Dong et al.

JOURNAL OF CONTROLLED RELEASE (2020)

Review Chemistry, Medicinal

Design and discovery of boronic acid drugs

Jessica Plescia et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

Review Chemistry, Medicinal

Anticancer boron-containing prodrugs responsive to oxidative stress from the tumor microenvironment

Hichem Maslah et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

Review Biochemistry & Molecular Biology

Pivotal role of boron supplementation on bone health: A narrative review

Mariangela Rondanelli et al.

JOURNAL OF TRACE ELEMENTS IN MEDICINE AND BIOLOGY (2020)

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Evaluation of the Anti-cancer and Biological Effects of Boric Acid on Colon Cancer Cell Line

Ayse Cigel et al.

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Use of mechanistic information to derive chemical-specific adjustment factors - Refinement of risk assessment

C. Smeraldi et al.

REGULATORY TOXICOLOGY AND PHARMACOLOGY (2020)

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Preclinical study of boron neutron capture therapy for bone metastasis using human breast cancer cell lines

Tooru Andoh et al.

APPLIED RADIATION AND ISOTOPES (2020)

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Boron in drug design: Recent advances in the development of new therapeutic agents

Guilherme Felipe Santos Fernandes et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

Article Oncology

Estimating the global cancer incidence and mortality in 2018: GLOBOCAN sources and methods

J. Ferlay et al.

INTERNATIONAL JOURNAL OF CANCER (2019)

Article Chemistry, Medicinal

Enhanced Tumor Selectivity of 5-Fluorouracil Using a Reactive Oxygen Species-Activated Prodrug Approach

Yong Ai et al.

ACS MEDICINAL CHEMISTRY LETTERS (2019)

Review Chemistry, Multidisciplinary

Boronic acids as building blocks for the construction of therapeutically useful bioconjugates

Joao P. M. Antonio et al.

CHEMICAL SOCIETY REVIEWS (2019)

Review Biochemistry & Molecular Biology

Prodrug strategies for targeted therapy triggered by reactive oxygen species

Jorge Peiro Cadahia et al.

MEDCHEMCOMM (2019)

Article Engineering, Environmental

Self-immolative chemistry in nanomedicine

M. Gisbert-Garzaran et al.

CHEMICAL ENGINEERING JOURNAL (2018)

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Small molecule KDM4s inhibitors as anti-cancer agents

Hongzhi Lin et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2018)

Article Biochemistry & Molecular Biology

Zinc binding groups for histone deacetylase inhibitors

Lei Zhang et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2018)

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The safety of bortezomib for the treatment of multiple myeloma

Guldane Cengiz Seval et al.

EXPERT OPINION ON DRUG SAFETY (2018)

Article Oncology

Tumor Mutation Burden as a Biomarker in Resected Non-Small-Cell Lung Cancer

Siddhartha Devarakonda et al.

JOURNAL OF CLINICAL ONCOLOGY (2018)

Review Pharmacology & Pharmacy

The preclinical discovery and development of bortezomib for the treatment of mantle cell lymphoma

Richard Arkwright et al.

EXPERT OPINION ON DRUG DISCOVERY (2017)

Article Chemistry, Medicinal

Urea-containing peptide boronic acids as potent proteasome inhibitors

Li-Qiang Han et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2017)

Review Chemistry, Multidisciplinary

Ratiometric Fluorescent Probes for the Detection of Reactive Oxygen Species

Diana Andina et al.

CHEMISTRY-A EUROPEAN JOURNAL (2017)

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Assessment of 10B concentration in boron neutron capture therapy: potential of image-guided therapy using 18FBPA PET

Eku Shimosegawa et al.

ANNALS OF NUCLEAR MEDICINE (2016)

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Ixazomib: First Global Approval

Matt Shirley

Article Chemistry, Medicinal

Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1

Sabin Llona-Minguez et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

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Alcohol, Aldehyde, and Ketone Liberation and Intracellular Cargo Release through Peroxide-Mediated α-Boryl Ether Fragmentation

Ramsey D. Hanna et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2016)

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Boronic prodrug of endoxifen as an effective hormone therapy for breast cancer

Changde Zhang et al.

BREAST CANCER RESEARCH AND TREATMENT (2015)

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Disturbing Trends in Physician Burnout and Satisfaction With Work-Life Balance: Dealing With Malady Among the Nation's Healers

Dan Ariely et al.

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An Activatable Prodrug for the Treatment of Metastatic Tumors

Eun-Joong Kim et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2014)

Article Biochemistry & Molecular Biology

Update on human health effects of boron

Forrest H. Nielsen

JOURNAL OF TRACE ELEMENTS IN MEDICINE AND BIOLOGY (2014)

Article Chemistry, Multidisciplinary

Substituent Effects on Oxidation-Induced Formation of Quinone Methides from Arylboronic Ester Precursors

Sheng Cao et al.

CHEMISTRY-A EUROPEAN JOURNAL (2013)

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Drug rechallenge and treatment beyond progression-implications for drug resistance

Elizabeth A. Kuczynski et al.

NATURE REVIEWS CLINICAL ONCOLOGY (2013)

Article Chemistry, Medicinal

Boron-Containing Compounds as Preventive and Chemotherapeutic Agents for Cancer

Romulus I. Scorei et al.

Anti-Cancer Agents in Medicinal Chemistry (2012)

Article Chemistry, Medicinal

Boronate Probes as Diagnostic Tools for Real Time Monitoring of Peroxynitrite and Hydroperoxides

Jacek Zielonka et al.

CHEMICAL RESEARCH IN TOXICOLOGY (2012)

Article Chemistry, Multidisciplinary

Disclosing the Structure/Activity Correlation in Trivalent Boron-Containing Compounds: A Tendency Map

Jessica Cid et al.

CHEMISTRY-A EUROPEAN JOURNAL (2012)

Article Chemistry, Inorganic & Nuclear

New classes of carborane-appended 5-thio-D-glucopyranose derivatives

Rashmirekha Satapathy et al.

DALTON TRANSACTIONS (2012)

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Dietary boron: Progress in establishing essential roles in human physiology

Curtiss D. Hunt

JOURNAL OF TRACE ELEMENTS IN MEDICINE AND BIOLOGY (2012)

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ROS-activated anticancer prodrugs: a new strategy for tumor-specific damage

Xiaohua Peng et al.

THERAPEUTIC DELIVERY (2012)

Article Biochemistry & Molecular Biology

Calcium Fructoborate-Potential Anti-inflammatory Agent

Romulus Ion Scorei et al.

BIOLOGICAL TRACE ELEMENT RESEARCH (2011)

Article Biochemistry & Molecular Biology

Effect of Boron on Osteogenic Differentiation of Human Bone Marrow Stromal Cells

Xiaozhou Ying et al.

BIOLOGICAL TRACE ELEMENT RESEARCH (2011)

Review Pharmacology & Pharmacy

Principles of early drug discovery

J. P. Hughes et al.

BRITISH JOURNAL OF PHARMACOLOGY (2011)

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Hydrogen Peroxide Inducible DNA Cross-Linking Agents: Targeted Anticancer Prodrugs

Yunyan Kuang et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2011)

Article Biochemistry & Molecular Biology

Comparative effects of daily and weekly boron supplementation on plasma steroid hormones and proinflammatory cytokines

Mohammad Reza Naghii et al.

JOURNAL OF TRACE ELEMENTS IN MEDICINE AND BIOLOGY (2011)

Article Chemistry, Medicinal

Boron-containing phenoxyacetanilide derivatives as hypoxia-inducible factor (HIF)-1α inhibitors

Kazuki Shimizu et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2010)

Review Pharmacology & Pharmacy

Building on bortezomib: second-generation proteasome inhibitors as anti-cancer therapy

Lawrence R. Dick et al.

DRUG DISCOVERY TODAY (2010)

Article Oncology

Risk of colorectal cancer in men on long-term androgen deprivation therapy for prostate cancer

Silke Gillessen et al.

JOURNAL OF THE NATIONAL CANCER INSTITUTE (2010)

Article Pathology

Estrogen and Xenoestrogens in Breast Cancer

S. V. Fernandez et al.

TOXICOLOGIC PATHOLOGY (2010)

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The proteasome: Overview of structure and functions

Keiji Tanaka

PROCEEDINGS OF THE JAPAN ACADEMY SERIES B-PHYSICAL AND BIOLOGICAL SCIENCES (2009)

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Potent and selective peptidyl boronic acid inhibitors of the serine protease Prostate-Specific Antigen

Aaron M. LeBeau et al.

CHEMISTRY & BIOLOGY (2008)

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Boron intake and prostate cancer risk

Alejandro Gonzalez et al.

CANCER CAUSES & CONTROL (2007)

Article Pharmacology & Pharmacy

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EXPERT OPINION ON INVESTIGATIONAL DRUGS (2007)

Article Biochemistry & Molecular Biology

The role of estrogen in the initiation of breast cancer

J. Russo et al.

JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY (2006)

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Boron neutron capture therapy of cancer: Current status and future prospects

RF Barth et al.

CLINICAL CANCER RESEARCH (2005)

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Boric acid inhibits human prostate cancer cell proliferation

WT Barranco et al.

CANCER LETTERS (2004)

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Synthesis and evaluation of oxazaborolidines for antibacterial activity against Streptococcus mutans

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JOURNAL OF MEDICINAL CHEMISTRY (2004)

Article Surgery

Men with colorectal cancer are predisposed to prostate cancer

AR Moot et al.

ANZ JOURNAL OF SURGERY (2003)

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Current status of the molecular genetics of human prostatic adenocarcinomas

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INTERNATIONAL JOURNAL OF CANCER (2003)