ArticleDalton transactions (Cambridge, England : 2003)2012
Bioactive cyclometalated phthalimides: design, synthesis and kinase inhibition.
Article in Dalton transactions (Cambridge, England : 2003), 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
6 citing papers in PubMed.
- Azolium Control of the Osmium-Promoted Aromatic C-H Bond Activation in 1,3-Disubstituted Substrates.Organometallics · 2021Article
- Expanding medicinal chemistry into 3D space: metallofragments as 3D scaffolds for fragment-based drug discovery.Chemical science · 2019Article
- An iridium(iii)-based irreversible protein-protein interaction inhibitor of BRD4 as a potent anticancer agent.Chemical science · 2015Article
- An organometallic inhibitor for the human repair enzyme 7,8-dihydro-8-oxoguanosine triphosphatase.Angewandte Chemie (International ed. in English) · 2014Article
- Non-ATP-Mimetic Organometallic Protein Kinase Inhibitor.ChemistryOpen · 2013Article
- Mirror-image organometallic osmium arene iminopyridine halido complexes exhibit similar potent anticancer activity.Chemistry (Weinheim an der Bergstrasse, Germany) · 2013Article
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
The regioselective cyclometalation of 4-(pyridin-2-yl)phthalimide was exploited for the economical design of organometallic protein kinase inhibitors. 4-(Pyridin-2-yl)phthalimide can be prepared from inexpensive 4-bromophthalimide in just three steps including one Pd-catalyzed Stille cross-coupling. The versatility of this new ligand was demonstrated with the synthesis of ruthenium(II) half-sandwich as well as octahedral ruthenium(II) and iridium(III) complexes. The regioselectivity of the C-H activation in the course of the cyclometalation can be influenced by the reaction conditions and the steric demand of the introduced metal complex fragment. The biological activity of this new class of metalated phthalimides was evaluated by profiling two representative members against a large panel of human protein kinases. A cocrystal structure of one metallo-phthalimide with the protein kinase Pim1 confirmed an ATP-competitive binding with the intended hydrogen bonding between the phthalimide moiety and the hinge region of the ATP-binding site.
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Registered trials
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