ArticleInorganic chemistry2022
Developing Metal-Binding Isosteres of 8-Hydroxyquinoline as Metalloenzyme Inhibitor Scaffolds.
Article in Inorganic chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 22 citations in OpenAlex.
- Design and Biological Evaluation of Mannich-Modified 8-Hydroxyquinoline-Phthalimide Hybrids Against Drug-Resistant Cancer Cells.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Selective Synthesis of Imidazo[4,5‑ACS omega · 2025Article
- Upcycling waste zirconia block dental powders: towards a facile and highly selective on-off optical probe for sensing ZnRSC advances · 2025Article
- BRD4354 Is a Potent Covalent Inhibitor against the SARS-CoV-2 Main Protease.Biochemistry · 2024Article
- Development of Human Carbonic Anhydrase II Heterobifunctional Degraders.Journal of medicinal chemistry · 2023Article
- Masking thiol reactivity with thioamide, thiourea, and thiocarbamate-based MBPs.Chemical communications (Cambridge, England) · 2023Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The use of metal-binding pharmacophores (MBPs) in fragment-based drug discovery has proven effective for targeted metalloenzyme drug development. However, MBPs can still suffer from pharmacokinetic liabilities. Bioisostere replacement is an effective strategy utilized by medicinal chemists to navigate these issues during the drug development process. The quinoline pharmacophore and its bioisosteres, such as quinazoline, are important building blocks in the design of new therapeutics. More relevant to metalloenzyme inhibition, 8-hydroxyquinoline (8-HQ) and its derivatives can serve as MBPs for metalloenzyme inhibition. In this report, 8-HQ isosteres are designed and the coordination chemistry of the resulting metal-binding isosteres (MBIs) is explored using a bioinorganic model complex. In addition, the physicochemical properties and metalloenzyme inhibition activity of these MBIs were investigated to establish drug-like profiles. This report provides a new group of 8-HQ-derived MBIs that can serve as novel scaffolds for metalloenzyme inhibitor development with tunable, and potentially improved, physicochemical properties.
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Registered trials
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