Journal article
Triazole-based inhibitors of geranylgeranyltransferase II
Bioorganic & medicinal chemistry letters, Vol.23(3), pp.764-766
02/01/2013
DOI: 10.1016/j.bmcl.2012.11.089
PMID: 23266123
Abstract
A small set of triazole bisphosphonates has been prepared and tested for the ability to inhibit geranylgeranyltransferase II (GGTase II). The compounds were prepared through use of click chemistry to assemble a central triazole that links a polar head group to a hydrophobic tail. The resulting compounds were tested for their ability to inhibit GGTase II in an in vitro enzyme assay and also were tested for cytotoxic activity in an MTT assay with the human myeloma RPMI-8226 cell line. The most potent enzyme inhibitor was the triazole with a geranylgeranyl tail, which suggests that inhibitors that can access the enzyme region that holds the isoprenoid tail will display greater activity.
Details
- Title: Subtitle
- Triazole-based inhibitors of geranylgeranyltransferase II
- Creators
- Xiang Zhou - Department of Chemistry, University of Iowa, Iowa City, IA 52242-1294, USASara V Hartman - Department of Internal Medicine, University of Iowa, Iowa City, IA 52242-1294, USAElla J Born - Department of Internal Medicine, University of Iowa, Iowa City, IA 52242-1294, USAJacqueline P Smits - Department of Chemistry, University of Iowa, Iowa City, IA 52242-1294, USASarah A Holstein - Department of Internal Medicine, University of Iowa, Iowa City, IA 52242-1294, USADavid F Wiemer - Department of Chemistry, University of Iowa, Iowa City, IA 52242-1294, USA
- Resource Type
- Journal article
- Publication Details
- Bioorganic & medicinal chemistry letters, Vol.23(3), pp.764-766
- DOI
- 10.1016/j.bmcl.2012.11.089
- PMID
- 23266123
- NLM abbreviation
- Bioorg Med Chem Lett
- ISSN
- 0960-894X
- eISSN
- 1464-3405
- Publisher
- Elsevier Ltd
- Language
- English
- Date published
- 02/01/2013
- Academic Unit
- Neuroscience and Pharmacology; Chemistry
- Record Identifier
- 9983985981502771
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