In vivo evaluation of substituted 3-phenyl,7-methoxy-benzopyrans as modified estrogens

Abstract

AbstractSubstituted 3-phenyl,7-methoxy-benzopyran derivatives and vitamin D 3 (cholecalciferol, 1) were evaluated for their estrogen agonistic and antagonistic activities in immature female Sprague-Dawley rat model. The benzopyran derivatives 17 and 18, which were made as hybrids of estrogen and vitamin D 3 (pseudo vitamin D 3 analogs), showed significant estrogen agonistic activity (up to 48%) and weak estrogen antagonistic activity (up to 6%) at 10 mg/kg, whereas vitamin D 3 showed significant estrogen agonistic (82%) and antagonistic activities (39%) at 10 mg/kg.Graphical abstractSubstituted 3-phenyl, 7-methoxy-benzopyran derivavtives and vitamin-D3 (Cholecalciferol, 1) wereevaluated for their estrogen agonistic and antagonistic activities in mature female Sprague-Dawley ratmodel. The benzopyran derivatives, which were made as hybrids of estrogen and vitamin-D3 (pseudovitamin-D3 analogs), showed significant estrogen agonistic activity (upto 48%) and weak estrogenantagonistic activity (upto 6%) at 10 mg kg -1 . Whereas, vitamin-D3 showed significant estrogenagonistic (82%) and antagonistic activities (39%) at 10 mg kg -1 .[IMAGE]