ArticleBioorganic & medicinal chemistry2012
Development of a new class of aromatase inhibitors: design, synthesis and inhibitory activity of 3-phenylchroman-4-one (isoflavanone) derivatives.
Article in Bioorganic & medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 56 citations in OpenAlex.
- Pharmacophoric Investigation of a Natural Product-like Class of Aromatase Inhibitors Using Molecular Modeling.ACS omega · 2026Article
- Eco-friendly Approaches to Chromene Derivatives: A Comprehensive Review of Green Synthesis Strategies.Current topics in medicinal chemistry · 2025Review
- Advantages and Disadvantages of TwoTurkish journal of pharmaceutical sciences · 2022Article
- Synthesis, Docking Studies and Biological Activity of New Benzimidazole- Triazolothiadiazine Derivatives as Aromatase Inhibitor.Molecules (Basel, Switzerland) · 2020Article
- Estrogen alpha receptor antagonists for the treatment of breast cancer: a review.Chemistry Central journal · 2018Review
- 3D-QSAR study of steroidal and azaheterocyclic human aromatase inhibitors using quantitative profile of protein-ligand interactions.Journal of cheminformatics · 2018Article
- Binding mode of triazole derivatives as aromatase inhibitors based on docking, protein ligand interaction fingerprinting, and molecular dynamics simulation studies.Research in pharmaceutical sciences · 2017Article
- Botanicals and Their Bioactive Phytochemicals for Women's Health.Pharmacological reviews · 2016Review
- Recent Progress in the Discovery of Next Generation Inhibitors of Aromatase from the Structure-Function Perspective.Journal of medicinal chemistry · 2016Review
- Chemoprevention of Breast Cancer by Dietary Polyphenols.Molecules (Basel, Switzerland) · 2015Review
- Investigation of fluorinated and bifunctionalized 3-phenylchroman-4-one (isoflavanone) aromatase inhibitors.Bioorganic & medicinal chemistry · 2014Article
- Article
- Novel inhibitor discovery against aromatase through virtual screening and molecular dynamic simulation: a computational approach in drug design.EXCLI journal · 2013Article
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
Abstract
Aromatase (CYP19) catalyzes the aromatization reaction of androgen substrates to estrogens, the last and rate-limiting step in estrogen biosynthesis. Inhibition of aromatase is a new and promising approach to treat hormone-dependent breast cancer. We present here the design and development of isoflavanone derivatives as potential aromatase inhibitors. Structural modifications were performed on the A and B rings of isoflavanones via microwave-assisted, gold-catalyzed annulation reactions of hydroxyaldehydes and alkynes. The in vitro aromatase inhibition of these compounds was determined by fluorescence-based assays utilizing recombinant human aromatase (baculovirus/insect cell-expressed). The compounds 3-(4-phenoxyphenyl)chroman-4-one (1h), 6-methoxy-3-phenylchroman-4-one (2a) and 3-(pyridin-3-yl)chroman-4-one (3b) exhibited potent inhibitory effects against aromatase with IC(50) values of 2.4 μM, 0.26 μM and 5.8 μM, respectively. Docking simulations were employed to investigate crucial enzyme/inhibitor interactions such as hydrophobic interactions, hydrogen bonding and heme iron coordination. This report provides useful information on aromatase inhibition and serves as a starting point for the development of new flavonoid aromatase inhibitors.
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Registered trials
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