Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds.

Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds. Research Abstract Details 

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Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds. Abstract Text:

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.

Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds. Publishing Authors By Initials

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Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 18

Page Numbers: 2628-32

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 1464-3405

DAY: 14

MONTH: 03

YEAR: 2008

Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

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Grant and Affiliation Information for Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds.

AFFILIATION: Department of Chemistry, Scripps Florida, 5353 Parkside Drive, RE-2, Jupiter, FL 33458, USA.

Country: England

AGENCY: United States NIMH

GRANT: U54MH074404

ACRONYM: MH

MEDLINETA: Bioorg Med Chem Lett

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