Synthesis and biological evaluation of a series of aromatic bisphosphonates.
Basic Information
ID: ALA1250542
Journal: Bioorg Med Chem
Title: Synthesis and biological evaluation of a series of aromatic bisphosphonates.
Authors: Barney RJ, Wasko BM, Dudakovic A, Hohl RJ, Wiemer DF.
Abstract: Geminal bisphosphonates display varied biological activity depending on the nature of the substituents on the central carbon atom. For example, the nitrogenous bisphosphonates zoledronate and risedronate inhibit the enzyme farnesyl diphosphate synthase while digeranyl bisphosphonate has been shown to inhibit the enzyme geranylgeranyl diphosphate synthase. We now have synthesized isoprenoid bisphosphonates where an aromatic ring has been used to replace one of the isoprenoid olefins in an isoprenoid bisphosphonate and investigated the ability of these new compounds to impair protein geranylgeranylation within cells. Several of these new compounds are potent inhibitors of the enzyme geranylgeranyl diphosphate synthase.
CiteXplore: 20832326
DOI: 10.1016/j.bmc.2010.08.036
Patent ID: ┄