Discovery, molecular modeling and biological evaluation of 1,3,5-triaril-pyrazole derivates as novel Estrogen Receptor Modulators

Abstract

The biological actions of estrogens are mediated by estrogen binding to one of two specific estrogen receptors (ERs), ERαand ERβ. The ERs,which belong to the nuclear receptor superfamily of ligand-regulated transcription factors, are products of different genes and exhibit tissue- andcell-type specific expression. Clinically relevant, ERs are currently considered relevant drug targets for prevention and/or treatment of several dis-eases (from cancer, metabolic and cardiovascular, inflammation, and osteoporosis to neurodegeneration). In this work, new derivatives of1,3,5-triaril-pyrazoles were designed, synthesized and evaluated in vitro as Estrogen Receptor Modulators.