Synthesis and study of benzofuran-pyran analogs as BMP-2 targeted osteogenic agents

European Journal of Medicinal Chemistry
Pragati KushwahaKoneni V Sashidhara

Abstract

Twenty-four novel benzofuran-pyran derivatives were synthesized and evaluated for their anti-osteoporotic activity in primary cultures of rat calvarial osteoblasts in vitro. Among all the compounds screened for the alkaline phosphatase activity, three compounds 4e, 4j and 4k showed potent activity at picomolar concentrations in osteoblast differentiating stimulation. Additionally, these compounds were found effective in mineralization, assessed by alizarin red-S staining assay. Compounds were again validated through a series of other in vitro experiments. Moreover, molecular dynamics simulations demonstrated that both benzofuran and pyran moieties are requisite to fit into the active site of BMP-2 receptor, a key target of the osteogenic agents. The obtained results strongly convey that compound 4e is a potential bone anabolic agent among synthesized series, which can be further explored as a drug lead for treating osteoporosis.

Citations

Sep 6, 2020·Acta Crystallographica. Section C, Structural Chemistry·Nguyen Tien CongLuc Van Meervelt
Sep 29, 2019·Expert Opinion on Therapeutic Patents·Kamal M Dawood
Apr 25, 2020·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Ashish Kumar TripathiRitu Trivedi
Jul 3, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mashooq A BhatAbdullah Al-Dhfyan
Feb 3, 2022·Apoptosis : an International Journal on Programmed Cell Death·Ashish Kumar TripathiRitu Trivedi

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