Synthesis of potent water-soluble tissue transglutaminase inhibitors

Martin Griffin; Alexandre Mongeot; Russell Collighan; Robert E. Saint; Richard A. Jones; Ian G.C. Coutts; Daniel L. Rathbone

doi:10.1016/j.bmcl.2008.09.006

Synthesis of potent water-soluble tissue transglutaminase inhibitors

Martin Griffin, Alexandre Mongeot, Russell Collighan, Robert E. Saint, Richard A. Jones, Ian G.C. Coutts, Daniel L. Rathbone

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67 Citations (Scopus)

Abstract

Dipeptide-based sulfonium peptidylmethylketones derived from 6-diazo-5-oxo-L-norleucine (DON) have been investigated as potential water-soluble inhibitors of extracellular transglutaminase. The lead compounds were prepared in four steps and exhibited potent activity against tissue transglutaminase.

Original language	English
Pages (from-to)	5559-5562
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	20
DOIs	https://doi.org/10.1016/j.bmcl.2008.09.006
Publication status	Published - 15 Oct 2008

Keywords

transglutaminase
inhibitors
dipeptide

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10.1016/j.bmcl.2008.09.006

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abstract = "Dipeptide-based sulfonium peptidylmethylketones derived from 6-diazo-5-oxo-L-norleucine (DON) have been investigated as potential water-soluble inhibitors of extracellular transglutaminase. The lead compounds were prepared in four steps and exhibited potent activity against tissue transglutaminase.",

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author = "Martin Griffin and Alexandre Mongeot and Russell Collighan and Saint, {Robert E.} and Jones, {Richard A.} and Coutts, {Ian G.C.} and Rathbone, {Daniel L.}",

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AU - Collighan, Russell

AU - Saint, Robert E.

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AU - Coutts, Ian G.C.

AU - Rathbone, Daniel L.

PY - 2008/10/15

Y1 - 2008/10/15

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AB - Dipeptide-based sulfonium peptidylmethylketones derived from 6-diazo-5-oxo-L-norleucine (DON) have been investigated as potential water-soluble inhibitors of extracellular transglutaminase. The lead compounds were prepared in four steps and exhibited potent activity against tissue transglutaminase.

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KW - inhibitors

KW - dipeptide

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DO - 10.1016/j.bmcl.2008.09.006

M3 - Article

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EP - 5562

JO - Bioorganic and Medicinal Chemistry Letters

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Synthesis of potent water-soluble tissue transglutaminase inhibitors

Abstract

Keywords

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