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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-Monzón, Roberto Marrero-Alonso, Jorge Díaz, Mario Fernández Pérez, Leandro Estévez-Braun, Ana |
UNESCO Clasification: | 32 Ciencias médicas 230207 Química clínica 2390 Química farmacéutica |
Keywords: | Activated Protein-Kinase Solvent-Free Conditions Molecular docking Selective modulation Estrogen receptors, et al |
Issue Date: | 2015 | 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. | URI: | http://hdl.handle.net/10553/48245 | ISSN: | 1860-7179 | DOI: | 10.1002/cmdc.201500148 | Source: | ChemMedChem [ISSN 1860-7179], v. 10 (8), p. 1403-1412 |
Appears in Collections: | Artículos |
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