P3 SAR exploration of biphenyl carbamate based Legumain inhibitors

Catherine Higgins, Samira Bouazzaoui, Kishore Gaddale Devanna, Zenobia D'Costa, Amy Templeman, Martin O'Rourke, Andrew Young, Christopher Scott, Tim Harrison, Paul Mullan, Rich Williams

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

This Letter describes the further development and SAR exploration of a novel series of Legumain inhibitors. Based upon a previously identified Legumain inhibitor from our group, we explored the SAR of the carbamate phenyl ring system to probe the P3 pocket of the enzyme. This led to the identification of a sub-nanomolar inhibitor of Legumain.

Original languageEnglish
Pages (from-to)2521-2524
JournalBioorganic and Medicinal Chemistry Letters
Volume24
Issue number11
Early online date12 Apr 2014
DOIs
Publication statusPublished - 01 Jun 2014

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asparaginylendopeptidase
Carbamates
Enzymes
diphenyl

Cite this

Higgins, Catherine ; Bouazzaoui, Samira ; Gaddale Devanna, Kishore ; D'Costa, Zenobia ; Templeman, Amy ; O'Rourke, Martin ; Young, Andrew ; Scott, Christopher ; Harrison, Tim ; Mullan, Paul ; Williams, Rich. / P3 SAR exploration of biphenyl carbamate based Legumain inhibitors. In: Bioorganic and Medicinal Chemistry Letters. 2014 ; Vol. 24, No. 11. pp. 2521-2524.
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P3 SAR exploration of biphenyl carbamate based Legumain inhibitors. / Higgins, Catherine; Bouazzaoui, Samira; Gaddale Devanna, Kishore; D'Costa, Zenobia; Templeman, Amy; O'Rourke, Martin; Young, Andrew; Scott, Christopher; Harrison, Tim; Mullan, Paul ; Williams, Rich.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 24, No. 11, 01.06.2014, p. 2521-2524.

Research output: Contribution to journalArticle

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AU - Higgins, Catherine

AU - Bouazzaoui, Samira

AU - Gaddale Devanna, Kishore

AU - D'Costa, Zenobia

AU - Templeman, Amy

AU - O'Rourke, Martin

AU - Young, Andrew

AU - Scott, Christopher

AU - Harrison, Tim

AU - Mullan, Paul

AU - Williams, Rich

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Higgins C, Bouazzaoui S, Gaddale Devanna K, D'Costa Z, Templeman A, O'Rourke M et al. P3 SAR exploration of biphenyl carbamate based Legumain inhibitors. Bioorganic and Medicinal Chemistry Letters. 2014 Jun 1;24(11):2521-2524. https://doi.org/10.1016/j.bmcl.2014.04.002