Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369942 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
The structure-based design, synthesis, and biological evaluation of two novel series of potent and selective MEK kinase inhibitors are described herein. The elaboration of a lead pyrrole derivative to a bicyclic dihydroindolone core provided compounds with high potency and good drug-like pharmaceutical properties. Further scaffold modification afforded a series of dihydroindolizinone inhibitors, including an orally available advanced preclinical MEK inhibitor with potent in vivo antitumor efficacy.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Mark E. Adams, Michael B. Wallace, Toufike Kanouni, Nicholas Scorah, Shawn M. O’Connell, Hiroshi Miyake, Lihong Shi, Petro Halkowycz, Lilly Zhang, Qing Dong,