Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 7, Pages 2048-2052Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.02.019
Keywords
Stearoyl CoA; Desaturase; SCD; HEPG2 assay; Microsomal assay; Pteridinone
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We identified a series of structurally novel SCD (Delta 9 desaturase) inhibitors via high-throughput screening and follow-up SAR studies. Modi. cation 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 Delta 5 and Delta 6 desaturases. (C) 2009 Elsevier Ltd. All rights reserved.
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