Development of a potent and selective cell penetrant Legumain inhibitor

Kerry A. Ness; Sharon L Eddie; Catherine A Higgins; Amy Templeman; Zenobia D'Costa; Kishore K.D. Gaddale; Samira Bouzzaoui; Linda Jordan; Dominic Janssen; Timothy Harrison; Frank Burkamp; Andrew Young; Roberta Burden; Christopher J Scott; Paul B Mullan; Rich Williams

doi:10.1016/j.bmcl.2015.10.001

Development of a potent and selective cell penetrant Legumain inhibitor

Kerry A. Ness, Sharon L Eddie, Catherine A Higgins, Amy Templeman, Zenobia D'Costa, Kishore K.D. Gaddale, Samira Bouzzaoui, Linda Jordan, Dominic Janssen, Timothy Harrison, Frank Burkamp, Andrew Young, Roberta Burden, Christopher J Scott, Paul B Mullan, Rich Williams

Research output: Contribution to journal › Article › peer-review

7 Citations (Scopus)

Abstract

This Letter describes the continued SAR exploration of small molecule Legumain inhibitors with the aim of developing a potent and selective in vitro tool compound. Work continued in this Letter explores the use of alternative P2-P3 linker units and the P3 group SAR which led to the identification of 10t, a potent, selective and cellularly active Legumain inhibitor. We also demonstrate that 10t has activity in both cancer cell viability and colony formation assays.

Original language	English
Pages (from-to)	5642-5645
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	25
Issue number	23
Early online date	09 Oct 2015
DOIs	https://doi.org/10.1016/j.bmcl.2015.10.001
Publication status	Published - 01 Dec 2015

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Roberta Burden
- r.burden@qub.ac.uk
- School of Pharmacy - Lecturer
- Material and Advanced Technologies for Healthcare
Person: Academic

Cite this

Ness, K. A., Eddie, S. L., Higgins, C. A., Templeman, A., D'Costa, Z., Gaddale, K. K. D., Bouzzaoui, S., Jordan, L., Janssen, D., Harrison, T., Burkamp, F., Young, A., Burden, R., Scott, C. J., Mullan, P. B., & Williams, R. (2015). Development of a potent and selective cell penetrant Legumain inhibitor. Bioorganic and Medicinal Chemistry Letters, 25(23), 5642-5645. https://doi.org/10.1016/j.bmcl.2015.10.001

Ness, Kerry A. ; Eddie, Sharon L ; Higgins, Catherine A ; Templeman, Amy ; D'Costa, Zenobia ; Gaddale, Kishore K.D. ; Bouzzaoui, Samira ; Jordan, Linda ; Janssen, Dominic ; Harrison, Timothy ; Burkamp, Frank ; Young, Andrew ; Burden, Roberta ; Scott, Christopher J ; Mullan, Paul B ; Williams, Rich. / Development of a potent and selective cell penetrant Legumain inhibitor. In: Bioorganic and Medicinal Chemistry Letters. 2015 ; Vol. 25, No. 23. pp. 5642-5645.

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title = "Development of a potent and selective cell penetrant Legumain inhibitor",

abstract = "This Letter describes the continued SAR exploration of small molecule Legumain inhibitors with the aim of developing a potent and selective in vitro tool compound. Work continued in this Letter explores the use of alternative P2-P3 linker units and the P3 group SAR which led to the identification of 10t, a potent, selective and cellularly active Legumain inhibitor. We also demonstrate that 10t has activity in both cancer cell viability and colony formation assays.",

author = "Ness, {Kerry A.} and Eddie, {Sharon L} and Higgins, {Catherine A} and Amy Templeman and Zenobia D'Costa and Gaddale, {Kishore K.D.} and Samira Bouzzaoui and Linda Jordan and Dominic Janssen and Timothy Harrison and Frank Burkamp and Andrew Young and Roberta Burden and Scott, {Christopher J} and Mullan, {Paul B} and Rich Williams",

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Ness, KA, Eddie, SL , Higgins, CA, Templeman, A, D'Costa, Z, Gaddale, KKD, Bouzzaoui, S, Jordan, L, Janssen, D, Harrison, T, Burkamp, F, Young, A , Burden, R , Scott, CJ , Mullan, PB & Williams, R 2015, 'Development of a potent and selective cell penetrant Legumain inhibitor', Bioorganic and Medicinal Chemistry Letters, vol. 25, no. 23, pp. 5642-5645. https://doi.org/10.1016/j.bmcl.2015.10.001

Development of a potent and selective cell penetrant Legumain inhibitor. / Ness, Kerry A.; Eddie, Sharon L ; Higgins, Catherine A; Templeman, Amy; D'Costa, Zenobia; Gaddale, Kishore K.D.; Bouzzaoui, Samira; Jordan, Linda; Janssen, Dominic; Harrison, Timothy; Burkamp, Frank; Young, Andrew ; Burden, Roberta ; Scott, Christopher J ; Mullan, Paul B ; Williams, Rich.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 25, No. 23, 01.12.2015, p. 5642-5645.

Research output: Contribution to journal › Article › peer-review

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AU - Eddie, Sharon L

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AU - Jordan, Linda

AU - Janssen, Dominic

AU - Harrison, Timothy

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AU - Young, Andrew

AU - Burden, Roberta

AU - Scott, Christopher J

AU - Mullan, Paul B

AU - Williams, Rich

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