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O-phenyl carbamate and phenyl urea thiiranes as selective matrix metalloproteinase-2 inhibitors that cross the blood-brain barrier.

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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Gooyit M,Song W,Mahasenan KV,Lichtenwalter K,Suckow MA,Schroeder VA,Wolter WR,Mobashery S,Chang M

doi

10.1021/jm401217d

subject

Has Abstract

pub_date

2013-10-24 00:00:00

pages

8139-50

issue

20

eissn

0022-2623

issn

1520-4804

journal_volume

56

pub_type

杂志文章

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