Synthesis and Evaluation of Structurally Diverse C-2-Substituted Thienopyrimidine-Based Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase
| Autor: | Hiu-Fung Lee, Cyrus M. Lacbay, Rebecca Boutin, Alexios N. Matralis, Jaeok Park, Daniel D. Waller, Tian Lai Guan, Michael Sebag, Youla S. Tsantrizos |
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| Rok vydání: | 2022 |
| Předmět: |
Male
Molecular Structure Antineoplastic Agents Bone Marrow Cells Saccharomyces cerevisiae Thiophenes Rats Fungal Proteins Mice Inbred C57BL Structure-Activity Relationship Pyrimidines Liver Geranylgeranyl-Diphosphate Geranylgeranyltransferase Drug Discovery Animals Humans Molecular Medicine Female Enzyme Inhibitors Multiple Myeloma Protein Binding |
| Zdroj: | Journal of Medicinal Chemistry. 65:2471-2496 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | Novel analogues of C-2-substituted thienopyrimidine-based bisphosphonates (C2-ThP-BPs) are described that are potent inhibitors of the human geranylgeranyl pyrophosphate synthase (hGGPPS). Members of this class of compounds induce target-selective apoptosis of multiple myeloma (MM) cells and exhibit antimyeloma activity |
| Databáze: | OpenAIRE |
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