Discovery of a novel benzopyranyl compound as a potent in vitro and in vivo osteogenic agent

Abstract

A novel osteogenic agent containing a benzopyranyl core skeleton was discovered from cell-based alkaline phosphatase (ALP) assay of a small-molecule library constructed by diversity-oriented synthetic approach. The subsequent structure–activity relationship study using ALP and TOPflash reporter gene assay confirmed 6b as an osteogenesis activator. In in vivo study, we successfully demonstrated that the oral treatment of ovariectomized mice with 6b resulted in increased bone mass and bone volume as well as improved bone quality.