Literature DB >> 19902964

Synthesis of biphenyl proteomimetics as estrogen receptor-alpha coactivator binding inhibitors.

Anna B Williams1, Patrick T Weiser, Robert N Hanson, Jillian R Gunther, John A Katzenellenbogen.   

Abstract

A novel series of biphenyl proteomimetic compounds were designed as estrogen receptor-alpha (ER(alpha)) coactivator binding inhibitors. Synthesis was accomplished through a convergent approach, employing Suzuki coupling chemistry to ligate the individual modular units. Initial biological results support the ability of these compounds to compete for the ER(alpha) coactivator binding groove.

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Year:  2009        PMID： 19902964      PMCID： PMC3263526          DOI： 10.1021/ol901999f

Source DB:  PubMed          Journal:  Org Lett        ISSN： 1523-7052            Impact factor:   6.005


  19 in total

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5.  Blocking estrogen signaling after the hormone: pyrimidine-core inhibitors of estrogen receptor-coactivator binding.

Authors:  Alexander A Parent; Jillian R Gunther; John A Katzenellenbogen
Journal:  J Med Chem       Date:  2008-09-12       Impact factor: 7.446

6.  Amphipathic benzenes are designed inhibitors of the estrogen receptor alpha/steroid receptor coactivator interaction.

Authors:  Jillian R Gunther; Terry W Moore; Margaret L Collins; John A Katzenellenbogen
Journal:  ACS Chem Biol       Date:  2008-05-16       Impact factor: 5.100

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Journal:  J Med Chem       Date:  2008-02-29       Impact factor: 7.446

8.  Synthesis and biological evaluation of a series of 1,1-dichloro-2,2,3-triarylcyclopropanes as pure antiestrogens.

Authors:  B W Day; R A Magarian; P T Jain; J T Pento; G K Mousissian; K L Meyer
Journal:  J Med Chem       Date:  1991-02       Impact factor: 7.446

9.  Synthesis and structure-activity relationship study of antidiabetic penta-O-galloyl-D-glucopyranose and its analogues.

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Journal:  J Med Chem       Date:  2006-05-04       Impact factor: 8.039

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  10 in total

Review 1.  Nuclear receptor coregulators: modulators of pathology and therapeutic targets.

Authors:  David M Lonard; Bert W O'Malley
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Review 2.  Steroid receptor/coactivator binding inhibitors: An update.

Authors:  Kornelia J Skowron; Kenneth Booker; Changfeng Cheng; Simone Creed; Brian P David; Phillip R Lazzara; Amy Lian; Zamia Siddiqui; Thomas E Speltz; Terry W Moore
Journal:  Mol Cell Endocrinol       Date:  2019-06-01       Impact factor: 4.102

3.  Synthesis of a tetrasubstituted tetrahydronaphthalene scaffold for α-helix mimicry via a MgBr2-catalyzed Friedel-Crafts epoxide cycloalkylation.

Authors:  Devan Naduthambi; Santosh Bhor; Michael B Elbaum; Neal J Zondlo
Journal:  Org Lett       Date:  2013-09-09       Impact factor: 6.005

4.  Reconfiguring the AR-TIF2 Protein-Protein Interaction HCS Assay in Prostate Cancer Cells and Characterizing the Hits from a LOPAC Screen.

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Journal:  Assay Drug Dev Technol       Date:  2016-09-08       Impact factor: 1.738

5.  Perfluoro-tert-butyl Homoserine Is a Helix-Promoting, Highly Fluorinated, NMR-Sensitive Aliphatic Amino Acid: Detection of the Estrogen Receptor·Coactivator Protein-Protein Interaction by 19F NMR.

Authors:  Caitlin M Tressler; Neal J Zondlo
Journal:  Biochemistry       Date:  2017-02-15       Impact factor: 3.162

6.  Nonsteroidal bivalent estrogen ligands: an application of the bivalent concept to the estrogen receptor.

Authors:  Min Shan; Kathryn E Carlson; Alexander Bujotzek; Anja Wellner; Ronald Gust; Marcus Weber; John A Katzenellenbogen; Rainer Haag
Journal:  ACS Chem Biol       Date:  2013-01-30       Impact factor: 5.100

7.  4,4'-Unsymmetrically substituted 3,3'-biphenyl alpha helical proteomimetics as potential coactivator binding inhibitors.

Authors:  Patrick T Weiser; Ching-Yi Chang; Donald P McDonnell; Robert N Hanson
Journal:  Bioorg Med Chem       Date:  2013-11-08       Impact factor: 3.641

8.  Molecular Pathways: Targeting Steroid Receptor Coactivators in Cancer.

Authors:  David M Lonard; Bert W O'Malley
Journal:  Clin Cancer Res       Date:  2016-09-21       Impact factor: 12.531

Review 9.  The Role of Steroid Receptor Coactivators in Hormone Dependent Cancers and Their Potential as Therapeutic Targets.

Authors:  Lei Wang; David M Lonard; Bert W O'Malley
Journal:  Horm Cancer       Date:  2016-04-28       Impact factor: 3.869

10.  In silico discovery and validation of potent small-molecule inhibitors targeting the activation function 2 site of human oestrogen receptor α.

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  10 in total

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