2-cyano-pyrimidines: A new chemotype for inhibitors of the cysteine protease cathepsin K

被引：35

作者：

Altmann, Eva ^{[1
]}

Aichholz, Reiner ^{[1
]}

Betschart, Claudia ^{[1
]}

Buhl, Thomas ^{[1
]}

Green, Jonathan ^{[1
]}

Irie, Osamu ^{[1
]}

Teno, Naoki ^{[1
]}

Lattmann, Rene ^{[1
]}

Tintelnot-Blomley, Marina ^{[1
]}

Missbach, Martin ^{[1
]}

机构：

[1] Novartis Inst BioMed Res, CH-4002 Basel, Switzerland

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 50卷 / 04期

关键词：

D O I：

10.1021/jm0613525

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Starting from the purine lead structure 1, a new series of cathepsin K inhibitors based on a pyrimidine scaffold have been explored. Investigations of P3 and P2 substituents based on molecular modeling suggestions resulted in potent cathepsin K inhibitors with an improved selectivity profile over other cathepsins.

引用

收藏

页码：591 / 594

页数：4

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