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 › Letter

6 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 languageEnglish
Pages (from-to)5642-5645
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number23
Early online date09 Oct 2015
DOIs
Publication statusPublished - 01 Dec 2015

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asparaginylendopeptidase
Assays
Cell Survival
Cells
Molecules
Neoplasms

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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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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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language = "English",
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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 › Letter

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

Y1 - 2015/12/1

N2 - 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.

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.

U2 - 10.1016/j.bmcl.2015.10.001

DO - 10.1016/j.bmcl.2015.10.001

M3 - Letter

C2 - 26522952

VL - 25

SP - 5642

EP - 5645

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 23

ER -

Ness KA, Eddie SL, Higgins CA, Templeman A, D'Costa Z, Gaddale KKD et al. Development of a potent and selective cell penetrant Legumain inhibitor. Bioorganic and Medicinal Chemistry Letters. 2015 Dec 1;25(23):5642-5645. https://doi.org/10.1016/j.bmcl.2015.10.001

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