| Literature DB >> 20236824 |
Ruo Xu1, David Cole, Ted Asberom, Tom Bara, Chad Bennett, Duane A Burnett, John Clader, Martin Domalski, William Greenlee, Lynn Hyde, Hubert Josien, Hongmei Li, Mark McBriar, Brian McKittrick, Andrew T McPhail, Dmitri Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgar Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Lili Zhang, Zhiqiang Zhao.
Abstract
A novel series of tricyclic gamma-secretase inhibitors was designed and synthesized via a conformational analysis of literature compounds. The preliminary results have shown that compounds in this new series have much improved in vitro potency and in vivo profiles. More importantly, they have greatly reduced Notch related toxicity that was associated with previous gamma-secretase inhibitors. Copyright 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID: 20236824 DOI: 10.1016/j.bmcl.2010.02.080
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823