ArticleCellular oncology (Dordrecht, Netherlands)2016
A novel curcumin-like dienone induces apoptosis in triple-negative breast cancer cells.
Article in Cellular oncology (Dordrecht, Netherlands), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 49 papers.
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Who cites it
49 citing papers in PubMed.
- A novel quinine derivative as a PIM-1 kinase inhibitor induces apoptosis via mitochondrial depolarization with selective cytotoxicity in acute lymphoblastic leukemia cells.Frontiers in pharmacology · 2026Article
- Functional Characterization of VS-186B, a Novel HDAC Inhibitor with Anticancer Activity.International journal of molecular sciences · 2025Article
- Novel 4-quinolone derivative inflicted cytotoxicity via intrinsic apoptotic pathway activation on human metastatic triple-negative breast cancer cells.Bioorganic chemistry · 2025Article
- Synthetic Curcumin Analogs in the Treatment of Cancer: A Literature Review.Current medicinal chemistry · 2025Review
- Article
- Discovery of new pyridine heterocyclic hybrids; design, synthesis, dynamic simulations, andRSC advances · 2023Article
- Oridonin Induces Apoptosis in Esophageal Squamous Cell Carcinoma by Inhibiting Cytoskeletal Protein LASP1 and PDLIM1.Molecules (Basel, Switzerland) · 2023Article
- Thiophene derivative inflicts cytotoxicity via an intrinsic apoptotic pathway on human acute lymphoblastic leukemia cells.PloS one · 2023Article
- Modified Curcumins as Potential Drug Candidates for Breast Cancer: An Overview.Molecules (Basel, Switzerland) · 2022Review
- Two novel piperidones induce apoptosis and antiproliferative effects on human prostate and lymphoma cancer cell lines.Investigational new drugs · 2022Article
- Mechanism-Based Sonodynamic-Chemo Combinations against Triple-Negative Breast Cancer.International journal of molecular sciences · 2022Article
- Identification of a Unique Cytotoxic Thieno[2,3-c]Pyrazole Derivative with Potent and Selective Anticancer Effects In Vitro.Biology · 2022Article
- Three novel piperidones exhibit tumor-selective cytotoxicity on leukemia cells via protein degradation and stress-mediated mechanisms.Pharmacological reports : PR · 2022Article
- Article
- Novel Combinatorial Strategy Using Thermal Inkjet Bioprinting, Chemotherapy, and Radiation on Human Breast Cancer Cells; an In-Vitro Cell Viability Assessment.Materials (Basel, Switzerland) · 2021Article
- Docosahexaenoic Acid Inhibits Cell Proliferation through a Suppression of c-Myc Protein in Pancreatic Ductal Adenocarcinoma Cells.Antioxidants (Basel, Switzerland) · 2021Article
- Design, Syntheses, and Bioevaluations of Some NovelMedicines (Basel, Switzerland) · 2021Article
- Recombinant human lactoferrin carrying humanized glycosylation exhibits antileukemia selective cytotoxicity, microfilament disruption, cell cycle arrest, and apoptosis activities.Investigational new drugs · 2021Article
- Synthesis, Molecular Docking and Preliminary Antileukemic Activity of 4-Methoxybenzyl Derivatives Bearing Imidazo[2,1-b][1,3,4]thiadiazole.Chemistry & biodiversity · 2021Article
- Dienone Compounds: Targets and Pharmacological Responses.Journal of medicinal chemistry · 2020Article
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
purposeAccording to the World Health Organization (WHO), breast cancer is the most common cancer affecting women worldwide. In the USA ~12.3 % of all women are expected to be diagnosed with various types of breast cancer, exhibiting varying degrees of therapeutic response rates. Therefore, the identification of novel anti-breast cancer drugs is of paramount importance.
methodsThe 1,5-diaryl-3-oxo-1,4-pentadienyl pharmacophore was incorporated into a number of cytotoxins. Three of the resulting dienones, 2a, 2b and 2c, were tested for their anti-neoplastic potencies in a variety of human breast cancer-derived cell lines, including the triple negative MDA-MB-231 cell line and its metastatic variant, using a live-cell bio-imaging method. Special emphasis was put on dienone 2c, since its anti-cancer activity and its mode of inflicting cell death have so far not been reported.
resultsWe found that all three dienones exhibited potent cytotoxicities towards the breast cancer-derived cell lines tested, whereas significantly lower toxicities were observed towards the non-cancerous human breast cell line MCF-10A. The dienones 2b and 2c exhibited the greatest selective cytotoxicity at submicromolar concentration levels. We found that these two dienones induced phosphatidylserine externalization in MDA-MB-231 cells in a concentration-dependent manner, suggesting that their cytotoxic effect might be mediated by apoptosis. This possibility was confirmed by our observation that the dienone 2c can induce mitochondrial depolarization, caspase-3 activation, cell cycle disruption and DNA fragmentation in MDA-MB-231 cells.
conclusionOur findings indicate that dienone 2c uses the mitochondrial/intrinsic pathway to inflict apoptosis in triple negative MDA-MB-231 breast cancer-derived cells. This observation warrants further assessment of dienone 2c as a potential anti-breast cancer drug.
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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.