Literature DB >> 17289385

Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha.

Kevin D Dykstra1, Liangqin Guo, Elizabeth T Birzin, Wanda Chan, Yi Tien Yang, Edward C Hayes, Carolyn A DaSilva, Lee-Yuh Pai, Ralph T Mosley, Bryan Kraker, Paula M D Fitzgerald, Frank DiNinno, Susan P Rohrer, James M Schaeffer, Milton L Hammond.   

Abstract

A novel class of indole ligands for estrogen receptor alpha have been discovered which exhibit potent affinity and high selectivity. Substitution of the bazedoxifene skeleton to the linker present in the HTS lead 1a provided 22b which was found to be 130-fold alpha-selective and acted as an antagonist of estradiol activity in uterine tissue and MCF-7 cancer cells.

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Year:  2007        PMID： 17289385     DOI： 10.1016/j.bmcl.2007.01.054

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


  9 in total

1.  Consensus Induced Fit Docking (cIFD): methodology, validation, and application to the discovery of novel Crm1 inhibitors.

Authors:  Ori Kalid; Dora Toledo Warshaviak; Sharon Shechter; Woody Sherman; Sharon Shacham
Journal:  J Comput Aided Mol Des       Date:  2012-09-30       Impact factor: 3.686

2.  In vitro and in silico approach to study the hormonal activities of the alternative plasticizer tri-(2-ethylhexyl) trimellitate TEHTM and its metabolites.

Authors:  Laurence Dahbi; Amaury Farce; Nicolas Kambia; Isabelle Séverin; Thierry Dine; Emmanuel Moreau; Valérie Sautou; Marie-Christine Chagnon
Journal:  Arch Toxicol       Date:  2022-01-28       Impact factor: 5.153

3.  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

4.  Identification of xenoestrogens in food additives by an integrated in silico and in vitro approach.

Authors:  Alessio Amadasi; Andrea Mozzarelli; Clara Meda; Adriana Maggi; Pietro Cozzini
Journal:  Chem Res Toxicol       Date:  2009-01       Impact factor: 3.739

5.  Motif-directed redesign of enzyme specificity.

Authors:  Benjamin Borgo; James J Havranek
Journal:  Protein Sci       Date:  2014-02-04       Impact factor: 6.725

6.  1,2,4-Triazine Sulfonamides: Synthesis by Sulfenamide Intermediates, In Vitro Anticancer Screening, Structural Characterization, and Molecular Docking Study.

Authors:  Danuta Branowska; Zbigniew Karczmarzyk; Ewa Wolińska; Waldemar Wysocki; Maja Morawiak; Zofia Urbańczyk-Lipkowska; Anna Bielawska; Krzysztof Bielawski
Journal:  Molecules       Date:  2020-05-16       Impact factor: 4.411

7.  Mitigating the Adverse Effects of Polychlorinated Biphenyl Derivatives on Estrogenic Activity via Molecular Modification Techniques.

Authors:  Wei He; Wenhui Zhang; Zhenhua Chu; Yu Li
Journal:  Int J Environ Res Public Health       Date:  2021-05-08       Impact factor: 3.390

Review 8.  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

9.  Synthesis of unsymmetrical disulfanes bearing 1,2,4-triazine scaffold and their in vitro screening towards anti-breast cancer activity.

Authors:  Danuta Branowska; Justyna Ławecka; Mariusz Sobiczewski; Zbigniew Karczmarzyk; Waldemar Wysocki; Ewa Wolińska; Ewa Olender; Barbara Mirosław; Alicja Perzyna; Anna Bielawska; Krzysztof Bielawski
Journal:  Monatsh Chem       Date:  2018-06-27       Impact factor: 1.451
  9 in total

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