Ness Kerry Anne, Eddie Sharon L, Burton Stephanie, Harrison Timothy, Mullan Paul, 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. 2016 Jan 15;26(2):413-416. doi: 10.1016/j.bmcl.2015.11.101. Epub 2015 Nov 28.
This letter describes the design, development and SAR exploration of a novel series of small legumain inhibitors. The SAR of a new small molecule legumain inhibitor chemotype was explored and found to have improved physiochemical properties compared to previously developed inhibitors within our group. However, further development of this series was found to be limited as the SAR was observed to be relatively flat.
这封信描述了一系列新型小分子豆球蛋白抑制剂的设计、开发及对其活性的探索。对一种新型小分子豆球蛋白抑制剂化学类型的活性进行了探索，发现与我们团队之前开发的抑制剂相比，其理化性质有所改善。然而，由于观察到该系列的活性相对单一，发现该系列的进一步开发受到限制。
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