ArticleJournal of medicinal chemistry2012
Investigation of chalcones as selective inhibitors of the breast cancer resistance protein: critical role of methoxylation in both inhibition potency and cytotoxicity.
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 32 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
32 citing papers in PubMed.
- Identification of the Acetamide-Chalcone Derivative That Selectively Inhibits ABCG2 Transport Activity.ACS omega · 2026Article
- Drugs inducing interstitial lung disease: in silico analysis of their structures and targets.Molecular medicine (Cambridge, Mass.) · 2026Article
- Cytotoxic Activity of Opopanax hispidus (Friv.) Griseb.: Characterization of a New Chalcone-type Compound.Chemistry & biodiversity · 2025Article
- Effects of Cholesterol on the Breast Cancer Resistance Protein: Studies through the Synthesis and Biological Evaluation of Chemical Tools.ChemMedChem · 2025Article
- The potential of the South African plant Tulbaghia Violacea Harv for the treatment of triple negative breast cancer.Scientific reports · 2025Article
- Magnolol derivatives as specific and noncytotoxic inhibitors of breast cancer resistance protein (BCRP/ABCG2).Bioorganic chemistry · 2024Article
- ATP-Binding Cassette Subfamily G Member 2 in Acute Myeloid Leukemia: A New Molecular Target?Biomedicines · 2024Review
- Design and Synthesis of Novel α-Methylchalcone Derivatives, Anti-Cervical Cancer Activity, and Reversal of Drug Resistance in HeLa/DDP Cells.Molecules (Basel, Switzerland) · 2023Article
- Characterization of Potent ABCG2 Inhibitor Derived from Chromone: From the Mechanism of Inhibition to Human Extracellular Vesicles for Drug Delivery.Pharmaceutics · 2023Article
- Article
- Structural and molecular characterization of lopinavir and ivermectin as breast cancer resistance protein (BCRP/ABCG2) inhibitors.EXCLI journal · 2023Article
- Design, Synthesis, anticancer evaluation and in silico studies of 2,4,6-trimethoxychalcone derivatives.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2023Article
- Two Important Anticancer Mechanisms of Natural and Synthetic Chalcones.International journal of molecular sciences · 2022Review
- Tetrahydroquinoline/4,5-Dihydroisoxazole Molecular Hybrids as Inhibitors of Breast Cancer Resistance Protein (BCRP/ABCG2).ChemMedChem · 2021Article
- Mechanistic basis of breast cancer resistance protein inhibition by new indeno[1,2-b]indoles.Scientific reports · 2021Article
- Licochalcone A Selectively Resensitizes ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Chemotherapeutic Drugs.Journal of natural products · 2020Article
- ADMET evaluation in drug discovery. 20. Prediction of breast cancer resistance protein inhibition through machine learning.Journal of cheminformatics · 2020Article
- Development of benzochalcone derivatives as selective CYP1B1 inhibitors and anticancer agents.MedChemComm · 2019Article
- Recent advances in the search of BCRP- and dual P-gp/BCRP-based multidrug resistance modulators.Cancer drug resistance (Alhambra, Calif.) · 2019Review
- Tariquidar-Related Chalcones and Ketones as ABCG2 Modulators.ACS medicinal chemistry letters · 2018Article
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
ABCG2 plays a major role in anticancer-drug efflux and related tumor multidrug resistance. Potent and selective ABCG2 inhibitors with low cytotoxicity were investigated among a series of 44 chalcones and analogues (1,3-diarylpropenones), by evaluating their inhibitory effect on the transport of mitoxantrone, a known ABCG2 substrate. Six compounds producing complete inhibition with IC(50) values below 0.5 μM and high selectivity for ABCG2 were identified. The number and position of methoxy substituents appeared to be critical for both inhibition and cytotoxicity. The best compounds, with potent inhibition and low toxicity, contained an N-methyl-1-indolyl (compound 38) or a 6'-hydroxyl-2',4'-dimethoxy-1-phenyl (compound 27) moiety (A-ring) and two methoxy groups at positions 2 and 6 of the 3-phenyl moiety (B-ring). Methoxy substitution contributed to inhibition at positions 3 and 5, but had a negative effect at position 4. Finally, methoxy groups at positions 3, 4, and 5 of the B-ring markedly increased cytotoxicity and, therefore, should be avoided.
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Registered trials
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