Document Detail


Design, synthesis, and biological evaluation of conformationally constrained analogues of naphthol AS-E as inhibitors of CREB-mediated gene transcription.
MedLine Citation:
PMID:  22458559     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Cyclic AMP response element binding protein (CREB) is often dysregulated in cancer cells and is an attractive cancer drug target. Previously, we described naphthol AS-E (1) as a small molecule inhibitor of CREB-mediated gene transcription. To understand its bioactive conformation, a series of conformationally constrained analogues of 1 were designed and synthesized. Biological evaluation of these analogues suggests that the global energy minimum of 1 is the likely bioactive conformation.
Authors:
Min Jiang; Bingbing X Li; Fuchun Xie; Frances Delaney; Xiangshu Xiao
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Publication Detail:
Type:  Evaluation Studies; Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't     Date:  2012-04-09
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  55     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2012 Apr 
Date Detail:
Created Date:  2012-06-14     Completed Date:  2012-07-17     Revised Date:  2013-06-26    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  4020-4     Citation Subset:  IM    
Affiliation:
Program in Chemical Biology, Oregon Health & Science University, 3181 SW Sam Jackson Park Road, Portland, Oregon, USA.
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MeSH Terms
Descriptor/Qualifier:
Animals
Cell Line
Cyclic AMP Response Element-Binding Protein / antagonists & inhibitors*
Drug Design
HEK293 Cells
Humans
Luciferases, Renilla / metabolism
Molecular Conformation
Naphthols / chemical synthesis*,  pharmacology
Static Electricity
Transcription, Genetic / drug effects*
Grant Support
ID/Acronym/Agency:
R01 GM087305/GM/NIGMS NIH HHS; R01 GM087305-02/GM/NIGMS NIH HHS; R01GM087305/GM/NIGMS NIH HHS
Chemical
Reg. No./Substance:
0/Cyclic AMP Response Element-Binding Protein; 0/Naphthols; 0/naphthol AS-E; EC 1.13.12.5/Luciferases, Renilla
Comments/Corrections

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