Flat SAR of P3-methylsulphonamide based small molecule legumain inhibitors

Kerry Anne Ness; Sharon L Eddie; Stephanie Burton; Timothy Harrison; Paul Mullan; Rich Williams

doi:10.1016/j.bmcl.2015.11.101

Flat SAR of P3-methylsulphonamide based small molecule legumain inhibitors

Kerry Anne Ness, Sharon L Eddie, Stephanie Burton, Timothy Harrison, Paul Mullan, Rich Williams

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

6 Citations (Scopus)

Abstract

This letter describes the design, development and SAR exploration of a novel series of small legumain inhibitors. The SAR of a new small molecule legumain inhibitor chemotype was explored and found to have improved physiochemical properties compared to previously developed inhibitors within our group. However, further development of this series was found to be limited as the SAR was observed to be relatively flat.

Original language	English
Pages (from-to)	413-6
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	26
Issue number	2
Early online date	28 Nov 2015
DOIs	https://doi.org/10.1016/j.bmcl.2015.11.101
Publication status	Published - 15 Jan 2016

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10.1016/j.bmcl.2015.11.101

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title = "Flat SAR of P3-methylsulphonamide based small molecule legumain inhibitors",

abstract = "This letter describes the design, development and SAR exploration of a novel series of small legumain inhibitors. The SAR of a new small molecule legumain inhibitor chemotype was explored and found to have improved physiochemical properties compared to previously developed inhibitors within our group. However, further development of this series was found to be limited as the SAR was observed to be relatively flat.",

author = "Ness, {Kerry Anne} and Eddie, {Sharon L} and Stephanie Burton and Timothy Harrison and Paul Mullan and Rich Williams",

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T1 - Flat SAR of P3-methylsulphonamide based small molecule legumain inhibitors

AU - Ness, Kerry Anne

AU - Eddie, Sharon L

AU - Burton, Stephanie

AU - Harrison, Timothy

AU - Mullan, Paul

AU - Williams, Rich

PY - 2016/1/15

Y1 - 2016/1/15

N2 - This letter describes the design, development and SAR exploration of a novel series of small legumain inhibitors. The SAR of a new small molecule legumain inhibitor chemotype was explored and found to have improved physiochemical properties compared to previously developed inhibitors within our group. However, further development of this series was found to be limited as the SAR was observed to be relatively flat.

AB - This letter describes the design, development and SAR exploration of a novel series of small legumain inhibitors. The SAR of a new small molecule legumain inhibitor chemotype was explored and found to have improved physiochemical properties compared to previously developed inhibitors within our group. However, further development of this series was found to be limited as the SAR was observed to be relatively flat.

U2 - 10.1016/j.bmcl.2015.11.101

DO - 10.1016/j.bmcl.2015.11.101

M3 - Article

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SN - 0960-894X

VL - 26

SP - 413

EP - 416

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 2

ER -

Flat SAR of P3-methylsulphonamide based small molecule legumain inhibitors

Abstract

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