Amides as bioisosteres of triazole-based geranylgeranyl diphosphate synthase inhibitors.
Basic Information
ID: ALA4725285
Journal: Bioorg Med Chem
Title: Amides as bioisosteres of triazole-based geranylgeranyl diphosphate synthase inhibitors.
Authors: Goetz DB,Varney ML,Wiemer DF,Holstein SA
Abstract: Geranylgeranyl diphosphate synthase (GGDPS) inhibitors are of potential therapeutic interest as a consequence of their activity against the bone marrow cancer multiple myeloma. A series of bisphosphonates linked to an isoprenoid tail through an amide linkage has been prepared and tested for the ability to inhibit GGDPS in enzyme and cell-based assays. The amides were designed as analogues to triazole-based GGDPS inhibitors. Several of the new compounds show GGDPS inhibitory activity in both enzyme and cell assays, with potency dependent on chain length and olefin stereochemistry.
CiteXplore: 32690260
DOI: 10.1016/j.bmc.2020.115604
Patent ID: ┄