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ID: ALA4312018

Journal: Bioorg Med Chem Lett

Title: Novel benzimidazole phosphonates as potential inhibitors of protein prenylation.

Authors: Bhuiyan NH, Varney ML, Wiemer DF, Holstein SA.

Abstract: Benzimidazole carboxyphosphonates and bisphosphonates have been prepared and evaluated for their activity as inhibitors of protein prenylation or isoprenoid biosynthesis. The nature of the phosphonate head group was found to dictate enzyme specificity. The lead carboxyphosphonate inhibits geranylgeranyl transferase II while its corresponding bisphosphonate analogue potently inhibits farnesyl diphosphate synthase. The most active inhibitors effectively disrupted protein prenylation in human multiple myeloma cells.

CiteXplore: 31699606

DOI: 10.1016/j.bmcl.2019.126757