ArticleParasites & vectors2016
Selenophene and thiophene-core estrogen receptor ligands that inhibit motility and development of parasitic stages of Haemonchus contortus.
Article in Parasites & vectors, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 11 citations in OpenAlex.
- Design, synthesis, and biological evaluation of novel 3-aryl-4-(3,4,5-trimethoxyphenyl)selenophene derivatives as new tubulin inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2025Article
- Prediction and Prioritisation of Novel Anthelmintic Candidates from Public Databases Using Deep Learning and Available Bioactivity Data Sets.International journal of molecular sciences · 2025Article
- Evaluation of Serum Supplementation on the Development ofInternational journal of molecular sciences · 2025Article
- Sex-the most underappreciated variable in research: insights from helminth-infected hosts.Veterinary research · 2022Review
- Screening of the 'Open Scaffolds' collection from Compounds Australia identifies a new chemical entity with anthelmintic activities against different developmental stages of the barber's pole worm and other parasitic nematodes.International journal for parasitology. Drugs and drug resistance · 2017Article
- Selenophenes: Introducing a New Element into the Core of Non-Steroidal Estrogen Receptor Ligands.ChemMedChem · 2017Article
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Authors and funding
10 authors at 5 institutions in 2 countries.
Funding
Abstract
backgroundParasitic worms represent a substantial disease burden in animals and humans worldwide. The control of parasitic roundworms (nematodes) relies heavily on the use of anthelmintic drugs. However, widespread drug resistance in nematodes seriously compromises the effectiveness of many anthelmintics around the world. Thus, there is a need to discover new drugs, with unique modes of action, against parasites.
methodsHere, we synthesised and tested 74 selective estrogen receptor modulators (SERMs) for in vitro-activity on parasitic larvae of Haemonchus contortus (barber's pole worm), one of the most important nematode pathogens of small ruminants (including sheep and goats) and a key representative of one of the largest groups of parasitic nematodes (the Strongylida) of animals. We also studied the morphology of treated and untreated larvae using scanning electron microscopy (SEM), and assessed the agonistic/antagonistic activity of SERMs in a human embryonic kidney cell line using a luciferase reporter assay system.
resultsWe identified three SERMs (one selenophene and two thiophene-core compounds) with potent inhibitory activities (at 3-25 μM) on the motility and development of parasitic stages of H. contortus. An SEM examination of treated H. contortus revealed considerable damage to the cuticle of fourth- but not exsheathed, third-stage larvae; this damage appeared to be consistent with that observed upon treatment with monepantel but not moxidectin (control compounds).
conclusionThe potency of the three SERMs compared favourably with commercially available anthelmintics, such that they warrant further assessment as nematocides. Future studies could focus on assessing the selectivity of these SERMs to parasites, characterising their target(s) and/or designing analogs that are parasite-specific.
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