1.
Bioorg Med Chem Lett
; 25(23): 5642-5, 2015 Dec 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-26522952
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.