Ness Kerry A, Eddie Sharon L, Higgins Catherine A, Templeman Amy, D'Costa Zenobia, Gaddale Kishore K D, Bouzzaoui Samira, Jordan Linda, Janssen Dominic, Harrison Timothy, Burkamp Frank, Young Andrew, Burden Roberta, Scott Christopher J, Mullan Paul B, Williams Rich
CCRCB Drug Discovery Group, Centre for Cancer Research and Cell Biology, Queen's University Belfast, 97 Lisburn Rd., Belfast BT9 7BL, UK.
Almac Discovery, Almac House, 20 Seagoe Industrial Estate, Craigavon BT63 5QD, UK.
Bioorg Med Chem Lett. 2015 Dec 1;25(23):5642-5. doi: 10.1016/j.bmcl.2015.10.001. Epub 2015 Oct 9.
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.
