ArticleJournal of medicinal chemistry2013
O-phenyl carbamate and phenyl urea thiiranes as selective matrix metalloproteinase-2 inhibitors that cross the blood-brain barrier.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 34 citations in OpenAlex.
- MMP-1 and ADAM10 as Targets for Therapeutic Intervention in Idiopathic Pulmonary Fibrosis.ACS pharmacology & translational science · 2022Article
- Metabolism of the Selective Matrix Metalloproteinase-9 Inhibitor (ACS pharmacology & translational science · 2021Article
- Limitations of Knockout Mice and Other Tools in Assessment of the Involvement of Matrix Metalloproteinases in Wound Healing and the Means to Overcome Them.ACS pharmacology & translational science · 2020Article
- In Search of Selectivity in Inhibition of ADAM10.ACS medicinal chemistry letters · 2018Article
- Exploitation of Conformational Dynamics in Imparting Selective Inhibition for Related Matrix Metalloproteinases.ACS medicinal chemistry letters · 2017Article
- 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
- Early Gelatinase Activity Is Not a Determinant of Long-Term Recovery after Traumatic Brain Injury in the Immature Mouse.PloS one · 2015Article
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Authors and funding
9 authors at 1 institution in 1 country.
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Abstract
Brain metastasis occurs in 20-40% of cancer patients. Treatment is mostly palliative, and the inability of most drugs to penetrate the brain presents one of the greatest challenges in the development of therapeutics for brain metastasis. Matrix metalloproteinase-2 (MMP-2) plays important roles in invasion and vascularization of the central nervous system and represents a potential target for treatment of brain metastasis. Carbonate, O-phenyl carbamate, urea, and N-phenyl carbamate derivatives of SB-3CT, a selective and potent gelatinase inhibitor, were synthesized and evaluated. The O-phenyl carbamate and urea variants were selective and potent inhibitors of MMP-2. Carbamate 5b was metabolized to the potent gelatinase inhibitor 2, which was present at therapeutic concentrations in the brain. In contrast, phenyl urea 6b crossed the blood-brain barrier, however, higher doses would result in therapeutic brain concentrations. Carbamate 5b and urea 6b show potential for intervention of MMP-2-dependent diseases such as brain metastasis.
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Registered trials
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