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Title: Synthesis of 4,4′-Diaminotriphenylmethanes with Potential Selective Estrogen Receptor Modulator (SERM)-like Activity
Authors: Guedes, Gema
Amesty, Ángel
Jiménez-Monzõn, Roberto
Marrero-Alonso, Jorge
Díaz, Mario 
Fernández-Pérez, Leandro 
Estévez-Braun, Ana
Keywords: Activated Protein-Kinase
Solvent-Free Conditions
Baeyer Condensation
Structure Elucidation
Aromatic-Aldehydes, et al
Issue Date: 2015
Publisher: 1860-7179
Project: "Evaluación Preclinica de Nuevas Estructuras Quimicas Diseñadas Para Inhibir la Ruta Oncogenica Jak-Stat O Como Moduladores Selectivos de Los Receptores Estrógenos" 
Journal: ChemMedChem 
Abstract: In this study, a series of new 4,4-diaminotriphenylmethanes was efficiently synthesized from aromatic aldehydes and 2,5-dimethoxybenzenamine under microwave irradiation in the presence of Sc(OTf)(3) as a catalyst. Antiproliferative activity was assessed by using the MCF-7 estrogen receptor (ER)-positive breast cancer cell line, and antagonist/agonist transcriptional activities were determined. Docking studies and competition studies of triphenylmethanes and radiolabeled estradiol determined that these compounds do not bind the ER, indicating that triphenylmethane-induced changes in proliferative and transcriptional activities differ from conventional mechanisms of action triggered by other selective ER modulators.
ISSN: 1860-7179
DOI: 10.1002/cmdc.201500148
Source: ChemMedChem[ISSN 1860-7179],v. 10, p. 1403-1412
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