二恶嗪三嗪类作为新型组织蛋白酶 K 抑制剂。

Dioxo-triazines as a novel series of cathepsin K inhibitors.

机构信息

Schering-Plough Corporation, Newhouse, Lanarkshire, ML1 5SH, Scotland, United Kingdom.

出版信息

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1488-90. doi: 10.1016/j.bmcl.2010.01.116. Epub 2010 Jan 25.

DOI:10.1016/j.bmcl.2010.01.116

PMID:20153187

Abstract

A novel dioxo-triazine series of cathepsin K inhibitors was identified from HTS. A rapid exploratory programme led to the discovery of potent and selective cathepsin K inhibitors, typified by compound 24 which displayed IC(50) values of 17nM against catK and >10,000nM in catL, catB and catS assays.

摘要

从高通量筛选中鉴定出一种新型的双氧三嗪系列组织蛋白酶 K 抑制剂。一个快速的探索性计划导致发现了有效的和选择性的组织蛋白酶 K 抑制剂，其中以化合物 24 为代表，其对 catK 的 IC50 值为 17nM，而在 catL、catB 和 catS 测定中大于 10000nM。