ArticlePloS one2015
Structure-activity relationships for the antifungal activity of selective estrogen receptor antagonists related to tamoxifen.
Article in PloS one, 2015. 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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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
16 citing papers in PubMed, 33 citations in OpenAlex.
- Beyond Conventional Antifungals: Combating Resistance Through Novel Therapeutic Pathways.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Progress of Antimicrobial Mechanisms of Stilbenoids.Pharmaceutics · 2024Review
- Discovery of new antimicrobial thiophene derivatives with activity against drug-resistant Gram negative-bacteria.Frontiers in pharmacology · 2024Article
- Development of an Imaging Flow Cytometry Method for Fungal Cytological Profiling and Its Potential Application in Antifungal Drug Development.Journal of fungi (Basel, Switzerland) · 2023Article
- The Pathological Activation of Microglia Is Modulated by Sexually Dimorphic Pathways.International journal of molecular sciences · 2023Review
- Antileishmanial Activity of Tamoxifen by Targeting Sphingolipid Metabolism: A Review.Clinical pharmacology : advances and applications · 2022Review
- Repurposing of the Tamoxifen Metabolites to Treat Methicillin-Resistant Staphylococcus epidermidis and Vancomycin-Resistant Enterococcus faecalis Infections.Microbiology spectrum · 2021Article
- Drug Repurposing in Medical Mycology: Identification of Compounds as Potential Antifungals to Overcome the Emergence of Multidrug-Resistant Fungi.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Repurposing of the Tamoxifen Metabolites to Combat Infections by Multidrug-Resistant Gram-Negative Bacilli.Antibiotics (Basel, Switzerland) · 2021Article
- Ospemifene displays broad-spectrum synergistic interactions with itraconazole through potent interference with fungal efflux activities.Scientific reports · 2020Article
- An inherent T cell deficit in healthy males to C. neoformans infection may begin to explain the sex susceptibility in incidence of cryptococcosis.Biology of sex differences · 2019Article
- Review
- An Overview of Sex Bias inJournal of fungi (Basel, Switzerland) · 2018Review
- Antifungal Phenothiazines: Optimization, Characterization of Mechanism, and Modulation of Neuroreceptor Activity.ACS infectious diseases · 2018Article
- Troponoids Can Inhibit Growth of the Human Fungal Pathogen Cryptococcus neoformans.Antimicrobial agents and chemotherapy · 2017Article
- New Horizons in Antifungal Therapy.Journal of fungi (Basel, Switzerland) · 2016Review
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
Cryptococcosis is one of the most important invasive fungal infections and is a significant contributor to the mortality associated with HIV/AIDS. As part of our program to repurpose molecules related to the selective estrogen receptor modulator (SERM) tamoxifen as anti-cryptococcal agents, we have explored the structure-activity relationships of a set of structurally diverse SERMs and tamoxifen derivatives. Our data provide the first insights into the structural requirements for the antifungal activity of this scaffold. Three key molecular characteristics affecting anti-cryptococcal activity emerged from our studies: 1) the presence of an alkylamino group tethered to one of the aromatic rings of the triphenylethylene core; 2) an appropriately sized aliphatic substituent at the 2 position of the ethylene moiety; and 3) electronegative substituents on the aromatic rings modestly improved activity. Using a cell-based assay of calmodulin antagonism, we found that the anti-cryptococcal activity of the scaffold correlates with calmodulin inhibition. Finally, we developed a homology model of C. neoformans calmodulin and used it to rationalize the structural basis for the activity of these molecules. Taken together, these data and models provide a basis for the further optimization of this promising anti-cryptococcal scaffold.
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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.