ArticleJournal of medicinal chemistry2011
Selective water-soluble gelatinase inhibitor prodrugs.
Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 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
20 citing papers in PubMed, 51 citations in OpenAlex.
- Therapeutic potential of inhibitors of gelatinases MMP-2 and MMP-9 for the treatment of breast cancer.The FEBS journal · 2026Review
- Matrix Metalloproteinase Inhibition in Melanoma.Experimental dermatology · 2026Review
- A Review of Immunomodulatory Reprogramming by Probiotics in Combating Chronic and Acute Diabetic Foot Ulcers (DFUs).Pharmaceutics · 2022Review
- Targeting Extracellular Matrix Remodeling Restores BRAF Inhibitor Sensitivity in BRAFi-resistant Melanoma.Clinical cancer research : an official journal of the American Association for Cancer Research · 2020Article
- Review
- Targeting MMP-9 in Diabetic Foot Ulcers.Pharmaceuticals (Basel, Switzerland) · 2019Review
- Mechanisms of Action of Novel Drugs Targeting Angiogenesis-Promoting Matrix Metalloproteinases.Frontiers in immunology · 2019Review
- Degradable polymer prodrugs with adjustable activity from drug-initiated radical ring-opening copolymerization.Chemical science · 2018Article
- The thiirane-based selective MT1-MMP/MMP2 inhibitor ND-322 reduces melanoma tumor growth and delays metastatic dissemination.Pharmacological research · 2016Article
- The Prodrug Approach: A Successful Tool for Improving Drug Solubility.Molecules (Basel, Switzerland) · 2015Review
- Acceleration of diabetic wound healing using a novel protease-anti-protease combination therapy.Proceedings of the National Academy of Sciences of the United States of America · 2015Article
- Water-Soluble MMP-9 Inhibitor Reduces Lesion Volume after Severe Traumatic Brain Injury.ACS chemical neuroscience · 2015Article
- Gd-Complexes of New Arylpiperazinyl Conjugates of DTPA-Bis(amides): Synthesis, Characterization and Magnetic Relaxation Properties.Molecules (Basel, Switzerland) · 2015Article
- Synthesis of mevalonate- and fluorinated mevalonate prodrugs and their in vitro human plasma stability.European journal of medicinal chemistry · 2015Article
- A chemical biological strategy to facilitate diabetic wound healing.ACS chemical biology · 2014Article
- O-phenyl carbamate and phenyl urea thiiranes as selective matrix metalloproteinase-2 inhibitors that cross the blood-brain barrier.Journal of medicinal chemistry · 2013Article
- Water-soluble mmp-9 inhibitor prodrug generates active metabolites that cross the blood-brain barrier.ACS chemical neuroscience · 2013Article
- Molecular design of a highly selective and strong protein inhibitor against matrix metalloproteinase-2 (MMP-2).The Journal of biological chemistry · 2013Article
- Structure-Activity Relationship for Thiirane-Based Gelatinase Inhibitors.ACS medicinal chemistry letters · 2012Article
- Matrix metalloproteinases in neuropathic pain and migraine: friends, enemies, and therapeutic targets.Pain research and treatment · 2012Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
SB-3CT (1), a selective and potent thiirane-based gelatinase inhibitor, is effective in animal models of cancer metastasis and stroke; however, it is limited by poor aqueous solubility and extensive metabolism. We addressed these issues by blocking the primary site of metabolism and capitalizing on a prodrug strategy to achieve >5000-fold increased solubility. The amide prodrugs were quantitatively hydrolyzed in human blood to a potent gelatinase inhibitor, ND-322 (3). The arginyl amide prodrug (ND-478, 5d) was metabolically stable in mouse, rat, and human liver microsomes. Both 5d and 3 were nonmutagenic in the Ames II mutagenicity assay. The prodrug 5d showed moderate clearance of 0.0582 L/min/kg, remained mostly in the extracellular fluid compartment (Vd = 0.0978 L/kg), and had a terminal half-life of >4 h. The prodrug 5d had superior pharmacokinetic properties than those of 3, making the thiirane class of selective gelatinase inhibitors suitable for intravenous administration in the treatment of acute gelatinase-dependent diseases.
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What OpenQuestion holds
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.