Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 8, Pages 2628-2632Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.03.027
Keywords
steroidogenic factor-1 (NR5A1); orphan nuclear receptor; isoquinolinone scaffold; SF-1 inhibitor; MLSCN
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Funding
- NIMH NIH HHS [U54 MH074404-03S1, U54MH074404, U54 MH074404, U54 MH084512] Funding Source: Medline
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Three synthetic routes were developed for structure-activity relationship (SAR) studies of HTS-derived isoquinolinone inhibitor probes for the orphan nuclear receptor steroidogenic factor-1 (NR5A1). Among the new analogs reported herein, 31 and 32 have improved potency, lower cellular toxicity, and improved selectivity compared to the initial HTS-derived leads 1 and 2. (c) 2008 Elsevier Ltd. All rights reserved.
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