ArticleBioorganic & medicinal chemistry letters2013
Triazole-based inhibitors of geranylgeranyltransferase II.
Article in Bioorganic & medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed.
- Incorporation of an alpha-hydroxy substituent modulates activity of triazole bisphosphonate-based geranylgeranyl diphosphate synthase inhibitors.Bioorganic & medicinal chemistry · 2026Article
- Structural Insight into Geranylgeranyl Diphosphate Synthase (GGDPS) for Cancer Therapy.Molecular cancer therapeutics · 2024Review
- Review
- Targeting the Isoprenoid Biosynthetic Pathway in Multiple Myeloma.International journal of molecular sciences · 2022Review
- Article
- ω-Hydroxy isoprenoid bisphosphonates as linkable GGDPS inhibitors.Bioorganic & medicinal chemistry letters · 2019Article
- Regulation of the Notch-ATM-abl axis by geranylgeranyl diphosphate synthase inhibition.Cell death & disease · 2019Article
- Synthesis of (1,2,3-triazol-4-yl)methyl Phosphinates and (1,2,3-Triazol-4-yl)methyl Phosphates by Copper-Catalyzed Azide-Alkyne Cycloaddition.Molecules (Basel, Switzerland) · 2019Article
- Recent Advances in the Development of Mammalian Geranylgeranyl Diphosphate Synthase Inhibitors.Molecules (Basel, Switzerland) · 2017Review
- Antitrypanosomal and antileishmanial activity of prenyl-1,2,3-triazoles.MedChemComm · 2017Article
- Bishomoisoprenoid triazole bisphosphonates as inhibitors of geranylgeranyl diphosphate synthase.Bioorganic & medicinal chemistry · 2017Article
- Olefin Isomers of a Triazole Bisphosphonate Synergistically Inhibit Geranylgeranyl Diphosphate Synthase.Molecular pharmacology · 2017Article
- Stereoselective Synthesis of Homoneryl and Homogeranyl Triazole Bisphosphonates.The Journal of organic chemistry · 2016Article
- A new motif for inhibitors of geranylgeranyl diphosphate synthase.Bioorganic & medicinal chemistry · 2016Article
- Stereocontrolled regeneration of olefins from epoxides.Tetrahedron letters · 2016Article
- Evolutionary comparison of prenylation pathway in kinetoplastid Leishmania and its sister Leptomonas.BMC evolutionary biology · 2015Article
- N-Oxide derivatives of 3-(3-pyridyl)-2-phosphonopropanoic acids as potential inhibitors of Rab geranylgeranylation.Bioorganic & medicinal chemistry letters · 2015Article
- Geranyl and neryl triazole bisphosphonates as inhibitors of geranylgeranyl diphosphate synthase.Bioorganic & medicinal chemistry · 2014Article
Corrections and comments
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Authors and funding
6 authors.
Funding
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.
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Registered trials
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