Abstract
| 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 | |
| Publication status | Published - 01 Jun 2014 |
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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
TY - JOUR
T1 - P3 SAR exploration of biphenyl carbamate based Legumain inhibitors
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
PY - 2014/6/1
Y1 - 2014/6/1
N2 - 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.
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.
U2 - 10.1016/j.bmcl.2014.04.002
DO - 10.1016/j.bmcl.2014.04.002
M3 - Article
VL - 24
SP - 2521
EP - 2524
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 11
ER -