Literature DB >> 18722117

Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands.

Jing Fang1, Adwoa Akwabi-Ameyaw, Jonathan E Britton, Subba R Katamreddy, Frank Navas, Aaron B Miller, Shawn P Williams, David W Gray, Lisa A Orband-Miller, Jean Shearin, Dennis Heyer.   

Abstract

A series of estrogen receptor ligands based on a 3-alkyl naphthalene scaffold was synthesized using an intramolecular enolate-alkyne cycloaromatization as the key step. Several of these compounds bearing a C6-OH group were shown to be high affinity ligands. All compounds had similar ERalpha and ERbeta binding affinity ranging from micromolar to low nanomolar.

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Year:  2008        PMID: 18722117     DOI: 10.1016/j.bmcl.2008.07.121

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  Human Estrogen Receptor Alpha Antagonists, Part 3: 3-D Pharmacophore and 3-D QSAR Guided Brefeldin A Hit-to-Lead Optimization toward New Breast Cancer Suppressants.

Authors:  Nezrina Kurtanović; Nevena Tomašević; Sanja Matić; Elenora Proia; Manuela Sabatino; Lorenzo Antonini; Milan Mladenović; Rino Ragno
Journal:  Molecules       Date:  2022-04-28       Impact factor: 4.927

2.  Identification of putative estrogen receptor-mediated endocrine disrupting chemicals using QSAR- and structure-based virtual screening approaches.

Authors:  Liying Zhang; Alexander Sedykh; Ashutosh Tripathi; Hao Zhu; Antreas Afantitis; Varnavas D Mouchlis; Georgia Melagraki; Ivan Rusyn; Alexander Tropsha
Journal:  Toxicol Appl Pharmacol       Date:  2013-05-23       Impact factor: 4.219

3.  Novel Biphenyl Amines Inhibit Oestrogen Receptor (ER)-α in ER-Positive Mammary Carcinoma Cells.

Authors:  Basappa Basappa; Baburajeev Chumadathil Pookunoth; Mamatha Shinduvalli Kempasiddegowda; Rangappa Knchugarakoppal Subbegowda; Peter E Lobie; Vijay Pandey
Journal:  Molecules       Date:  2021-02-03       Impact factor: 4.411

Review 4.  Versatility or promiscuity: the estrogen receptors, control of ligand selectivity and an update on subtype selective ligands.

Authors:  Hui Wen Ng; Roger Perkins; Weida Tong; Huixiao Hong
Journal:  Int J Environ Res Public Health       Date:  2014-08-26       Impact factor: 3.390

5.  Novel Promising Estrogenic Receptor Modulators: Cytotoxic and Estrogenic Activity of Benzanilides and Dithiobenzanilides.

Authors:  Malgorzata Kucinska; Maria-Dolores Giron; Hanna Piotrowska; Natalia Lisiak; Walter H Granig; Francisco-Javier Lopez-Jaramillo; Rafael Salto; Marek Murias; Thomas Erker
Journal:  PLoS One       Date:  2016-01-05       Impact factor: 3.240

  5 in total

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