ArticleCancer biology & therapy2011
Potent genistein derivatives as inhibitors of estrogen receptor alpha-positive breast cancer.
Article in Cancer biology & therapy, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 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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Who cites it
16 citing papers in PubMed, 62 citations in OpenAlex.
- Article
- Daidzein and Genistein: Natural Phytoestrogens with Potential Applications in Hormone Replacement Therapy.International journal of molecular sciences · 2025Review
- Unleashing the potential of Genistein and its derivatives as effective therapeutic agents for breast cancer treatment.Naunyn-Schmiedeberg's archives of pharmacology · 2025Review
- Gen inhibiting the Wnt/CaScientific reports · 2025Article
- Isoflavone Derivatives as Potential Anticancer Agents: Synthesis and Bioactivity Studies.ChemMedChem · 2024Review
- Tailoring Potential Natural Compounds for the Treatment of Luminal Breast Cancer.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Synthesis and Chemopreventive Potential of 5-FU/Genistein Hybrids on Colorectal Cancer Cells.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Thiogenistein-Antioxidant Chemistry, Antitumor Activity, and Structure Elucidation of New Oxidation Products.International journal of molecular sciences · 2022Article
- Natural Polyphenols in Metabolic Syndrome: Protective Mechanisms and Clinical Applications.International journal of molecular sciences · 2021Review
- Chinese Medicines Improve Perimenopausal Symptoms Induced by Surgery, Chemoradiotherapy, or Endocrine Treatment for Breast Cancer.Frontiers in pharmacology · 2019Review
- Estrogen alpha receptor antagonists for the treatment of breast cancer: a review.Chemistry Central journal · 2018Review
- Dietary Isoflavones and Breast Cancer Risk.Medicines (Basel, Switzerland) · 2017Review
- Preliminary in vitro evaluation of genistein chemopreventive capacity as a result of esterification and cyclodextrin encapsulation.Analytical cellular pathology (Amsterdam) · 2015Article
- Combating malaria with plant molecules: a brief update.Current medicinal chemistry · 2014Review
- Derailed estrogen signaling and breast cancer: an authentic couple.Endocrine reviews · 2013Review
- Cancer control and prevention by nutrition and epigenetic approaches.Antioxidants & redox signaling · 2012Review
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
The estrogen receptor (ER) is a major target for the treatment of breast cancer cells. Genistein, a soy isoflavone, possesses a structure similar to estrogen and can both mimic and antagonize estrogen effects although at high concentrations it inhibits breast cancer cell proliferation. Hence, to enhance the anti-cancer activity of Genistein at lower concentrations, we have synthesized seven structurally modified derivatives of Genistein (MA-6, MA-8, MA-11, MA-19, MA-20, MA-21 and MA-22) based on the structural requirements for an optimal anti-cancer effect. Among those seven, three derivatives (MA-6, MA-8 and MA-19) showed high antiproliferative activity with IC(50) levels in the range of 1-2.5 μM, i.e., at much lower concentrations range than Genistein itself, in three ER-positive breast cancer cell lines (MCF-7, 21PT and T47D) studied. In our analysis, we noticed that at IC(50) concentrations, the MA-6, MA-8 and MA-19 Genistein derivatives induced apoptosis, inhibited ER-α messenger RNA expression and increased the ratio of ER-β to ER-α levels in a manner comparable to the parent compound Genistein. Of note, these three modified Genistein derivatives exerted their effects at concentrations 10-15 times lower than the parent compound, decreasing the likelihood of significant ER- α pathway activation, which has been a concern for Genistein. Hence these compounds might play a useful role in breast cancer chemoprevention.
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Registered trials
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.