期刊
INORGANICA CHIMICA ACTA
卷 377, 期 1, 页码 34-41出版社
ELSEVIER SCIENCE SA
DOI: 10.1016/j.ica.2011.07.032
关键词
Metal-based drugs; Protein kinases; Inhibitors; Phosphine ligands; Ruthenium
Metal complexes have emerged as promising and novel scaffolds for the design of enzyme inhibitors. Reported herein are the design, synthesis, and evaluation of protein kinase inhibition properties of pyridocarbazole half-sandwich complexes containing P-donor ligands. The nature of the monodentate P-donor ligand has a strong effect on protein kinase binding properties, most likely due to a direct interaction with the glycine-rich loop in the ATP-binding site. We furthermore discovered that PMe3 pyridocarbazole complexes are interesting lead structures for the design of potent inhibitors for the protein kinase TrkA for which we obtained a nanomolar organometallic inhibitor. (C) 2011 Elsevier B. V. All rights reserved.
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