ArticleEuropean journal of medicinal chemistry2020
Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors.
Article in European journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 26 citations in OpenAlex.
- Green Knoevenagel condensation of indolin-2-one derivatives using undivided electrochemical cell.MethodsX · 2026Article
- Amoeboid cancer cells at a glance.Journal of cell science · 2026Review
- The structural requirements of 3,5-substituted oxindoles that determine selective AMPK or GSK3β inhibition.RSC medicinal chemistry · 2026Article
- Small Molecule Modulators of AMP-Activated Protein Kinase (AMPK) Activity and Their Potential in Cancer Therapy.Journal of medicinal chemistry · 2025Review
- Synthesis and Evaluation of Thiazolyl-indole-2-carboxamide Derivatives as Potent Multitarget Anticancer Agents.ACS omega · 2024Article
- Knockdown of EIF2AK2-OAS1 axis reduces ATP production inducing AMPK phosphorylation to inhibit the malignant behavior of gastric cancer cells.Journal of bioenergetics and biomembranes · 2024Article
- A Novel AMPK Inhibitor Sensitizes Pancreatic Cancer Cells to Ferroptosis Induction.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Is It Possible to Obtain a Product of the Desired Configuration from a Single Knoevenagel Condensation? Isomerization vs. Stereodefined Synthesis.International journal of molecular sciences · 2023Article
- A switchable redox annulation of 2-nitroarylethanols affordingChemical science · 2022Article
- The potent AMPK inhibitor BAY-3827 shows strong efficacy in androgen-dependent prostate cancer models.Cellular oncology (Dordrecht, Netherlands) · 2021Article
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Authors and funding
6 authors at 1 institution in 1 country.
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Abstract
AMP-activated protein kinase (AMPK) is a central metabolic regulator that promotes cancer growth and survival under hypoxia and plays a role in the maintenance of cancer stem cells. A major challenge to interrogating the potential of targeting AMPK in cancer is the lack of potent and selective small molecule inhibitors. Compound C has been widely used as an AMPK inhibitor, but it lacks potency and has a poor selectivity profile. The multi-kinase inhibitor, sunitinib, has demonstrated potent nanomolar inhibition of AMPK activity and has scope for modification. Here, we have designed and synthesized several series of oxindoles to determine the structural requirements for AMPK inhibition and to improve selectivity. We identified two potent, novel oxindole-based AMPK inhibitors that were designed to interact with the DFG motif in the ATP-binding site of AMPK, this key feature evades interaction with the common recptor tyrosine kinase targets of sunitinib. Cellular engagement of AMPK by these oxindoles was confirmed by the inhibition of phosphorylation of acetyl-CoA carboxylase (ACC), a known substrate of AMPK, in myeloid leukemia cells. Interestingly, although AMPK is highly expressed and activated in K562 cells these oxindole-based AMPK inhibitors did not impact cell viability or result in significant cytotoxicity. Our studies serve as a platform for the further development of oxindole-based AMPK inhibitors with therapeutic potential.
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