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

doi:10.1016/j.bmcl.2014.04.002

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 journal › Article

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 language	English
Pages (from-to)	2521-2524
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	24
Issue number	11
Early online date	12 Apr 2014
DOIs	https://doi.org/10.1016/j.bmcl.2014.04.002
Publication status	Published - 01 Jun 2014

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Higgins, C., Bouazzaoui, S., Gaddale Devanna, K., D'Costa, Z., Templeman, A., O'Rourke, M., Young, A., Scott, C., Harrison, T., Mullan, P., & Williams, R. (2014). P3 SAR exploration of biphenyl carbamate based Legumain inhibitors. Bioorganic and Medicinal Chemistry Letters, 24(11), 2521-2524. https://doi.org/10.1016/j.bmcl.2014.04.002

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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.",

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

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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 journal › Article

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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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AB - 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.

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DO - 10.1016/j.bmcl.2014.04.002

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JO - Bioorganic and Medicinal Chemistry Letters

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