Development of a potent and selective cell penetrant Legumain inhibitor
| Data(s) |
01/12/2015
|
|---|---|
| Resumo |
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. |
| Identificador | |
| Idioma(s) |
eng |
| Direitos |
info:eu-repo/semantics/restrictedAccess |
| Fonte |
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 , vol 25 , no. 23 , pp. 5642-5645 . DOI: 10.1016/j.bmcl.2015.10.001 |
| Tipo |
article |
