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Updated: Dec 14, 2025

Preparation of Enantiopure Non-Activated Aziridines and Synthesis of Biemamide B, D, and epiallo-Isomuscarine
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Amides as bioisosteres of triazole-based geranylgeranyl diphosphate synthase inhibitors
Daniel B Goetz1, Michelle L Varney2, David F Wiemer3
1Department of Chemistry, University of Iowa, Iowa City, IA 52242-1294, USA.
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.
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