| Literature DB >> 19249203 |
Dmitry O Koltun1, 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.
Abstract
We identified a series of structurally novel SCD (Delta9 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 IC(50) value of 50 pM in a HEPG2 SCD assay and has been shown to be metabolically stable and selective against Delta5 and Delta6 desaturases.Entities:
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Year: 2009 PMID： 19249203 DOI： 10.1016/j.bmcl.2009.02.019
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823