ArticleMolecules (Basel, Switzerland)2017
Novel Selective Estrogen Receptor Ligand Conjugates Incorporating Endoxifen-Combretastatin and Cyclofenil-Combretastatin Hybrid Scaffolds: Synthesis and Biochemical Evaluation.
Article in Molecules (Basel, Switzerland), 2017. 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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Who cites it
16 citing papers in PubMed, 32 citations in OpenAlex.
- Cancer Cells Show Higher Sensitivity to Melatonin-Tamoxifen Drug Conjugates than to Combination of Melatonin and Tamoxifen.ACS omega · 2024Article
- Potential of covalently linked tamoxifen hybrids for cancer treatment: recent update.RSC medicinal chemistry · 2024Review
- Design, synthesis,RSC medicinal chemistry · 2024Article
- Anticancer Drug Conjugates Incorporating Estrogen Receptor Ligands.Pharmaceutics · 2022Review
- S-Equol enhances osteoblastic bone formation and prevents bone loss through OPG/RANKLFrontiers in nutrition · 2022Article
- Targeting Estrogen Receptor-Positive Breast Microtumors with Endoxifen-Conjugated, Hypoxia-Sensitive Polymersomes.ACS omega · 2021Article
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- More Than Resveratrol: New Insights into Stilbene-Based Compounds.Biomolecules · 2020Review
- Selective estrogen receptor modulators in the prevention of breast cancer in premenopausal women: a review.Translational cancer research · 2020Review
- Microwave-assisted efficient one-pot synthesis ofBeilstein journal of organic chemistry · 2020Article
- HybridInternational journal of molecular sciences · 2019Review
- Genistein Improves Skin Flap Viability in Rats: A Preliminary In Vivo and In Vitro Investigation.Molecules (Basel, Switzerland) · 2018Article
- Hybrid Molecules Composed of 2,4-Diamino-1,3,5-triazines and 2-Imino-Coumarins and Coumarins. Synthesis and Cytotoxic Properties.Molecules (Basel, Switzerland) · 2018Article
- Drug conjugates-an emerging approach to treat breast cancer.Pharmacology research & perspectives · 2018Review
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Nuclear receptors such as the estrogen receptors (ERα and ERβ) modulate the effects of the estrogen hormones and are important targets for design of innovative chemotherapeutic agents for diseases such as breast cancer and osteoporosis. Conjugate and bifunctional compounds which incorporate an ER ligand offer a useful method of delivering cytotoxic drugs to tissue sites such as breast cancers which express ERs. A series of novel conjugate molecules incorporating both the ER ligands endoxifen and cyclofenil-endoxifen hybrids covalently linked to the antimitotic and tubulin targeting agent combretastatin A-4 were synthesised and evaluated as ER ligands. A number of these compounds demonstrated pro-apoptotic effects, with potent antiproliferative activity in ER-positive MCF-7 breast cancer cell lines and low cytotoxicity. These conjugates displayed binding affinity towards ERα and ERβ isoforms at nanomolar concentrations e.g., the cyclofenil-amide compound
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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.