| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375311 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
We identified a series of structurally novel SCD (Δ9 desaturase) inhibitors via high-throughput screening and follow-up SAR studies. Modification of the central bicyclic scaffold has proven key to our potency optimization effort. The most potent analog (8g) had IC50 value of 50 pM in a HEPG2 SCD assay and has been shown to be metabolically stable and selective against Δ5 and Δ6 desaturases.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Dmitry O. Koltun, Eric Q. Parkhill, Natalya I. Vasilevich, Andrei I. Glushkov, Timur M. Zilbershtein, Alexei V. Ivanov, Andrew G. Cole, Ian Henderson, Nathan A. Zautke, Sandra A. Brunn, Nevena Mollova, Kwan Leung, Jeffrey W. Chisholm, Jeff Zablocki,