ArticleBioorganic & medicinal chemistry2013
Benzimidazole-2-one: a novel anchoring principle for antagonizing p53-Mdm2.
Article in Bioorganic & medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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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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Who cites it
5 citing papers in PubMed, 21 citations in OpenAlex.
- Rational drug design, synthesis, and biological evaluation of novel chiral tetrahydronaphthalene-fused spirooxindole as MDM2-CDK4 dual inhibitor against glioblastoma.Acta pharmaceutica Sinica. B · 2020Article
- Artificial Macrocycles.Synlett : accounts and rapid communications in synthetic organic chemistry · 2018Article
- Article
- Discovery of a Potent Allosteric Kinase Modulator by Combining Computational and Synthetic Methods.Angewandte Chemie (International ed. in English) · 2015Article
- Multicomponent reactions for de novo synthesis of BODIPY probes: in vivo imaging of phagocytic macrophages.Journal of the American Chemical Society · 2013Article
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Authors and funding
6 authors at 3 institutions in 5 countries.
Funding
Abstract
Herein we propose the benzimidazole-2-one substructure as a suitable tryptophan mimic and thus a reasonable starting point for the design of p53 Mdm2 antagonists. We devise a short multicomponent reaction route to hitherto unknown 2-(2-oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)acetamides by reacting mono N-carbamate protected phenylenediamine in a Ugi-3CR followed by base induced cyclisation. Our preliminary synthesis and screening results are presented here. The finding of the benzimidazolone moiety as a tryptophan replacement in mdm2 is significant as it offers access to novel scaffolds with potentially higher selectivity and potency and improved biological activities. Observing low μM affinities to mdm2 by NMR and fluorescence polarization we conclude that the 2-(2-oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)acetamide scaffold might be a good starting point to further optimize the affinities to Mdm2.
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Registered trials
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