P3 SAR exploration of biphenyl carbamate based Legumain inhibitors


Autoria(s): 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
Data(s)

01/06/2014

Resumo

<br/>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.<br/><br/><br/><br/>Graphical abstract<br/><br/>

Identificador

http://pure.qub.ac.uk/portal/en/publications/p3-sar-exploration-of-biphenyl-carbamate-based-legumain-inhibitors(198765cd-5c16-4edc-b163-156a2ab677ee).html

http://dx.doi.org/10.1016/j.bmcl.2014.04.002

Idioma(s)

eng

Direitos

info:eu-repo/semantics/restrictedAccess

Fonte

Higgins , C , Bouazzaoui , S , Gaddale Devanna , K , D'Costa , Z , Templeman , A , O'Rourke , M , Young , A , Scott , C , Harrison , T , Mullan , P & Williams , R 2014 , ' P3 SAR exploration of biphenyl carbamate based Legumain inhibitors ' Bioorganic & Medicinal Chemistry , vol 24 , no. 11 , pp. 2521-2524 . DOI: 10.1016/j.bmcl.2014.04.002

Tipo

article