ArticleJournal of medicinal chemistry2012
Synthesis and evaluation of indole-based chalcones as inducers of methuosis, a novel type of nonapoptotic cell death.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 59 papers.
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Who cites it
59 citing papers in PubMed, 173 citations in OpenAlex.
- Tegavivint triggers TECR-dependent nonapoptotic cancer cell death.Nature chemical biology · 2025Article
- Macropinocytosis: Both a Target and a Tool for Cancer Therapy.Biomolecules · 2025Review
- Cell-Specific Vulnerability of Human Glioblastoma and Astrocytoma Cells to Mephedrone-An In Vitro Study.Molecules (Basel, Switzerland) · 2025Article
- Design, synthesis and antiviral activity of indole derivatives containing quinoline moiety.Molecular diversity · 2025Article
- Repurposing methuosis-inducing anticancer drugs for anthelmintic therapy.PLoS pathogens · 2024Review
- Forms of Non-Apoptotic Cell Death and Their Role in Gliomas-Presentation of the Current State of Knowledge.Biomedicines · 2024Review
- Studies on Autophagy and Apoptosis of Fibrosarcoma HT-1080 Cells Mediated by Chalcone with Indole Moiety.International journal of molecular sciences · 2024Article
- Synthesis, andCurrent computer-aided drug design · 2024Article
- Tanshinlactone triggers methuosis in breast cancer cells via NRF2 activation.Frontiers in pharmacology · 2024Article
- Design, Synthesis, and Evaluation of Novel Indole Hybrid Chalcones and Their Antiproliferative and Antioxidant Activity.Molecules (Basel, Switzerland) · 2023Article
- Progress in the discovery and development of small molecule methuosis inducers.RSC medicinal chemistry · 2023Review
- Target-Based Anticancer Indole Derivatives for the Development of Anti-Glioblastoma Agents.Molecules (Basel, Switzerland) · 2023Review
- Surveying the landscape of emerging and understudied cell death mechanisms.Biochimica et biophysica acta. Molecular cell research · 2023Review
- The V-ATPases in cancer and cell death.Cancer gene therapy · 2022Review
- Novel dual inhibitor for targeting PIM1 and FGFR1 kinases inhibits colorectal cancer growthActa pharmaceutica Sinica. B · 2022Article
- The autophagy inducer trehalose stimulates macropinocytosis in NF1-deficient glioblastoma cells.Cancer cell international · 2022Article
- Synthesis and Anti-Cancer Activity of New Pyrazolinyl-Indole Derivatives: Pharmacophoric Interactions and Docking Studies for Identifying New EGFR Inhibitors.International journal of molecular sciences · 2022Article
- Selectivity, Speciation, and Substrate Control in the Gold-Catalyzed Coupling of Indoles and Alkynes.Organometallics · 2022Article
- The Role and Therapeutic Potential of Macropinocytosis in Cancer.Frontiers in pharmacology · 2022Review
- Gilteritinib Enhances Anti-Tumor Efficacy of CDK4/6 Inhibitor, Abemaciclib in Lung Cancer Cells.Frontiers in pharmacology · 2022Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Methuosis is a novel caspase-independent form of cell death in which massive accumulation of vacuoles derived from macropinosomes ultimately causes cells to detach from the substratum and rupture. We recently described a chalcone-like compound, 3-(2-methyl-1H-indol-3-yl)-1-(4-pyridinyl)-2-propen-1-one (i.e., MIPP), which can induce methuosis in glioblastoma and other types of cancer cells. Herein, we describe the synthesis and structure-activity relationships of a directed library of related compounds, providing insights into the contributions of the two aryl ring systems and highlighting a potent derivative, 3-(5-methoxy, 2-methyl-1H-indol-3-yl)-1-(4-pyridinyl)-2-propen-1-one (i.e., MOMIPP) that can induce methuosis at low micromolar concentrations. We have also generated biologically active azide derivatives that may be useful for future studies aimed at identifying the protein targets of MOMIPP by photoaffinity labeling techniques. The potential significance of these studies is underscored by the finding that MOMIPP effectively reduces the growth and viability of Temozolomide-resistant glioblastoma and doxorubicin-resistant breast cancer cells. Thus, it may serve as a prototype for drugs that could be used to trigger death by methuosis in cancers that are resistant to conventional forms of cell death (e.g., apoptosis).
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.