Journal article
Amides as bioisosteres of triazole-based geranylgeranyl diphosphate synthase inhibitors
Bioorganic & medicinal chemistry, Vol.28(16), pp.115604-115604
08/15/2020
DOI: 10.1016/j.bmc.2020.115604
PMCID: PMC7384665
PMID: 32690260
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.
Details
- Title: Subtitle
- Amides as bioisosteres of triazole-based geranylgeranyl diphosphate synthase inhibitors
- Creators
- Daniel B Goetz - Department of Chemistry, University of Iowa, Iowa City, IA 52242-1294, USAMichelle L Varney - Department of Internal Medicine, University of Nebraska Medical Center, Omaha, NE 68198, USADavid F Wiemer - Department of Chemistry, University of Iowa, Iowa City, IA 52242-1294, USA; Department of Pharmacology, University of Iowa, Iowa City, IA 52242-1109, USASarah A Holstein - Department of Internal Medicine, University of Nebraska Medical Center, Omaha, NE 68198, USA. Electronic address: sarah.holstein@unmc.edu
- Resource Type
- Journal article
- Publication Details
- Bioorganic & medicinal chemistry, Vol.28(16), pp.115604-115604
- DOI
- 10.1016/j.bmc.2020.115604
- PMID
- 32690260
- PMCID
- PMC7384665
- NLM abbreviation
- Bioorg Med Chem
- ISSN
- 0968-0896
- eISSN
- 1464-3391
- Grant note
- P30 CA036727 / NCI NIH HHS P30 CA086862 / NCI NIH HHS
- Language
- English
- Date published
- 08/15/2020
- Academic Unit
- Neuroscience and Pharmacology; Chemistry
- Record Identifier
- 9984216693602771
Metrics
26 Record Views