ArticleJournal of medicinal chemistry2013
Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells.
Article in Journal of medicinal chemistry, 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.
- Exploration of a Novel Imidazo[4,5-b]pyridine-dihydropyrimidinone hybrids as aurora kinase a inhibitors: integrated pharmacophore modelling, docking and simulation approaches.Molecular diversity · 2026Article
- QSAR Study, Molecular Docking and Molecular Dynamic Simulation of Aurora Kinase Inhibitors Derived from Imidazo[4,5-Molecules (Basel, Switzerland) · 2024Article
- Recent Updates on Oncogenic Signaling of Aurora Kinases in Chemosensitive, Chemoresistant Cancers: Novel Medicinal Chemistry Approaches for Targeting Aurora Kinases.Current medicinal chemistry · 2024Review
- Design, synthesis, and biochemical and computational screening of novel oxindole derivatives as inhibitors of Aurora A kinase and SARS-CoV-2 spike/host ACE2 interaction.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2024Article
- α-Aminophosphonate inhibitors of metallo-β-lactamases NDM-1 and VIM-2.RSC medicinal chemistry · 2023Article
- Recent Advancement in Drug Design and Discovery of Pyrazole Biomolecules as Cancer and Inflammation Therapeutics.Molecules (Basel, Switzerland) · 2022Review
- 2-(3-Bromophenyl)-8-fluoroquinazoline-4-carboxylic Acid as a Novel and Selective Aurora A Kinase Inhibitory Lead with Apoptosis Properties: Design, Synthesis, In Vitro and In Silico Biological Evaluation.Life (Basel, Switzerland) · 2022Article
- CCT245718, a dual FLT3/Aurora A inhibitor overcomes D835Y-mediated resistance to FLT3 inhibitors in acute myeloid leukaemia cells.British journal of cancer · 2021Article
- Synthetic Strategies of Pyrimidine-Based Scaffolds as Aurora Kinase and Polo-like Kinase Inhibitors.Molecules (Basel, Switzerland) · 2021Review
- Design, synthesis and biological activity of NJournal of enzyme inhibition and medicinal chemistry · 2018Article
- Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.Molecules (Basel, Switzerland) · 2018Review
- Dynamic Equilibrium of the Aurora A Kinase Activation Loop Revealed by Single-Molecule Spectroscopy.Angewandte Chemie (International ed. in English) · 2017Article
- Azaindole synthesis through dual activation catalysis with N-heterocyclic carbenes.Chemical communications (Cambridge, England) · 2016Article
- 7-(Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the pyrazole N1-substituent.Bioorganic & medicinal chemistry letters · 2015Article
- The structure of C290A:C393A Aurora A provides structural insights into kinase regulation.Acta crystallographica. Section F, Structural biology communications · 2015Article
- A Cell Biologist's Field Guide to Aurora Kinase Inhibitors.Frontiers in oncology · 2015Article
- The azaindole framework in the design of kinase inhibitors.Molecules (Basel, Switzerland) · 2014Review
- Article
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20 authors.
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Abstract
Aurora-A differs from Aurora-B/C at three positions in the ATP-binding pocket (L215, T217, and R220). Exploiting these differences, crystal structures of ligand-Aurora protein interactions formed the basis of a design principle for imidazo[4,5-b]pyridine-derived Aurora-A-selective inhibitors. Guided by a computational modeling approach, appropriate C7-imidazo[4,5-b]pyridine derivatization led to the discovery of highly selective inhibitors, such as compound 28c, of Aurora-A over Aurora-B. In HCT116 human colon carcinoma cells, 28c and 40f inhibited the Aurora-A L215R and R220K mutants with IC50 values similar to those seen for the Aurora-A wild type. However, the Aurora-A T217E mutant was significantly less sensitive to inhibition by 28c and 40f compared to the Aurora-A wild type, suggesting that the T217 residue plays a critical role in governing the observed isoform selectivity for Aurora-A inhibition. These compounds are useful small-molecule chemical tools to further explore the function of Aurora-A in cells.
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