ArticleScientific reports2017
Identification of a novel chalcone derivative that inhibits Notch signaling in T-cell acute lymphoblastic leukemia.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 43 citations in OpenAlex.
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- Design and synthesis of novel chloropyridazine hybrids as promising anticancer agents acting by apoptosis induction and PARP-1 inhibition through a molecular hybridization strategy.RSC medicinal chemistry · 2024Article
- Selection of Natural Compounds with HMGA-Interfering Activities and Cancer Cell Cytotoxicity.ACS omega · 2023Article
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- Current Opportunities for Targeting Dysregulated Neurodevelopmental Signaling Pathways in Glioblastoma.Cells · 2022Review
- Synthesis and Antiproliferative Activity of Novel Dehydroabietic Acid-Chalcone Hybrids.Molecules (Basel, Switzerland) · 2022Article
- The Triprenylated Anthranoid Ferruginin A, a Promising Scaffold for the Development of Novel Antibiotics against Gram-Positive Bacteria.Antibiotics (Basel, Switzerland) · 2022Article
- Targeting Notch to Maximize Chemotherapeutic Benefits: Rationale, Advanced Strategies, and Future Perspectives.Cancers · 2021Review
- Identification of Effective Anticancer G-Quadruplex-Targeting Chemotypes through the Exploration of a High Diversity Library of Natural Compounds.Pharmaceutics · 2021Article
- Review
- Notch Signalling in Breast Development and Cancer.Frontiers in cell and developmental biology · 2021Review
- ASR490, a Small Molecule, Overrides Aberrant Expression ofMolecular cancer therapeutics · 2020Article
- Notch3 contributes to T-cell leukemia growth via regulation of the unfolded protein response.Oncogenesis · 2020Article
- Isolation and evaluation of cardenolides from Lansium domesticum as Notch inhibitors.Journal of natural medicines · 2020Article
- A novel colistin adjuvant identified by virtual screening for ArnT inhibitors.The Journal of antimicrobial chemotherapy · 2020Article
- Alvaxanthone, a Thymidylate Synthase Inhibitor with Nematocidal and Tumoricidal Activities.Molecules (Basel, Switzerland) · 2020Article
- The Revaluation of Plant-Derived Terpenes to Fight Antibiotic-Resistant Infections.Antibiotics (Basel, Switzerland) · 2020Review
- Structural Elucidation and Antimicrobial Characterization of Novel Diterpenoids fromACS medicinal chemistry letters · 2020Article
- Article
- Chalcones and Chalcone-mimetic Derivatives as Notch Inhibitors in a Model of T-cell Acute Lymphoblastic Leukemia.ACS medicinal chemistry letters · 2019Article
Corrections and comments
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Authors and funding
15 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Notch signaling is considered a rational target in the therapy of several cancers, particularly those harbouring Notch gain of function mutations, including T-cell acute lymphoblastic leukemia (T-ALL). Although currently available Notch-blocking agents are showing anti-tumor activity in preclinical studies, they are not effective in all the patients and often cause severe side-effects, limiting their widespread therapeutic use. Here, by functional and biological analysis of the most representative molecules of an in house library of natural products, we have designed and synthetized the chalcone-derivative 8 possessing Notch inhibitory activity at low micro molar concentration in T-ALL cell lines. Structure-activity relationships were afforded for the chalcone scaffold. Short term treatments with compound 8 resulted in a dose-dependent decrease of Notch signaling activity, halted cell cycle progression and induced apoptosis, thus affecting leukemia cell growth. Taken together, our data indicate that 8 is a novel Notch inhibitor, candidate for further investigation and development as an additional therapeutic option against Notch-dependent cancers.
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