ArticleJournal of medicinal chemistry2014
Reactive oxygen species (ROS) inducible DNA cross-linking agents and their effect on cancer cells and normal lymphocytes.
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
35 citing papers in PubMed, 106 citations in OpenAlex.
- Exploiting vitamin C as a prooxidant to activate ROS-responsive prodrugs for potent and selective tumor killing.Redox biology · 2026Article
- Tumor-Selective and Chemical Activation Strategies for Nitrogen Mustard Prodrugs.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Review
- Pharmacological investigation of bergapten isolated from Glehnia littoralis against periodontitis.Scientific reports · 2026Article
- HJournal of medicinal chemistry · 2025Article
- Recent Development of Boron-Containing Small-Molecule Anticancer Agents.ACS pharmacology & translational science · 2025Review
- Mechanistic Insights and Pharmacological Approaches for Nitrogen and Sulfur Mustards and Their Implications as Therapeutic Agents.Journal of applied toxicology : JAT · 2025Review
- Boronate-Based Bioactive Compounds Activated by Peroxynitrite and Hydrogen Peroxide.Redox biochemistry and chemistry · 2024Article
- Hydrogen peroxide responsive theranostics for cancer-selective activation of DNA alkylators and real-time fluorescence monitoring in living cells.European journal of medicinal chemistry · 2024Article
- Oxidative Stress and Age-Related Tumors.Antioxidants (Basel, Switzerland) · 2024Review
- Oxidative stress in the tumor microenvironment in gastric cancer and its potential role in immunotherapy.FEBS open bio · 2023Review
- Rhenium(V) Complexes as Cysteine-Targeting Coordinate Covalent Warheads.Journal of medicinal chemistry · 2023Article
- Design and synthesis of chromone-nitrogen mustard derivatives and evaluation of anti-breast cancer activity.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Synthesis of a boron-containing amidoxime reagent and its application to synthesize functionalized oxadiazole and quinazolinone derivatives.Tetrahedron letters · 2022Article
- Recent developments in the medicinal chemistry of single boron atom-containing compounds.Acta pharmaceutica Sinica. B · 2021Review
- Assessment of Phenylboronic Acid Nitrogen Mustards as Potent and Selective Drug Candidates for Triple-Negative Breast Cancer.ACS pharmacology & translational science · 2021Article
- Oxidative Stress in the Tumor Microenvironment and Its Relevance to Cancer Immunotherapy.Cancers · 2021Review
- Ferroptosis and Cancer: Complex Relationship and Potential Application of Exosomes.Frontiers in cell and developmental biology · 2021Review
- Development of Tumor-Targeting IRE-1 Inhibitors for B-cell Cancer Therapy.Molecular cancer therapeutics · 2020Article
- Hydrogen Peroxide Inducible JAK3 Covalent Inhibitor: Prodrug for the Treatment of RA with Enhanced Safety Profile.ACS medicinal chemistry letters · 2020Article
- Masked Phenolic-Selenium Conjugates: Potent and Selective Antiproliferative Agents Overcoming P-gp Resistance.Pharmaceuticals (Basel, Switzerland) · 2020Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
Reducing host toxicity is one of the main challenges of cancer chemotherapy. Many tumor cells contain high levels of ROS that make them distinctively different from normal cells. We report a series of ROS-activated aromatic nitrogen mustards that selectively kill chronic lymphocytic leukemia (CLL) over normal lymphocytes. These agents showed powerful DNA cross-linking abilities when coupled with H2O2, one of the most common ROS in cancer cells, whereas little DNA cross-linking was detected without H2O2. Consistent with chemistry observation, in vitro cytotoxicity assay demonstrated that these agents induced 40-80% apoptosis in primary leukemic lymphocytes isolated from CLL patients but less than 25% cell death to normal lymphocytes from healthy donors. The IC50 for the most potent compound (2) was ~5 μM in CLL cells, while the IC50 was not achieved in normal lymphocytes. Collectively, these data provide utility and selectivity of these agents that will inspire further and effective applications.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.