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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10.1016/j.bmcl.2015.10.001

Roberta Burden
- r.burdenqub.acuk
- School of Pharmacy - Lecturer
- Material and Advanced Technologies for Healthcare
Person: Academic

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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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doi = "10.1016/j.bmcl.2015.10.001",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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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

TY - JOUR

T1 - Development of a potent and selective cell penetrant Legumain inhibitor

AU - Ness, Kerry A.

AU - Eddie, Sharon L

AU - Higgins, Catherine A

AU - Templeman, Amy

AU - D'Costa, Zenobia

AU - Gaddale, Kishore K.D.

AU - Bouzzaoui, Samira

AU - Jordan, Linda

AU - Janssen, Dominic

AU - Harrison, Timothy

AU - Burkamp, Frank

AU - Young, Andrew

AU - Burden, Roberta

AU - Scott, Christopher J

AU - Mullan, Paul B

AU - Williams, Rich

PY - 2015/12/1

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AB - 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.

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DO - 10.1016/j.bmcl.2015.10.001

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EP - 5645

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 23

ER -

Development of a potent and selective cell penetrant Legumain inhibitor

Abstract

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