- Title
- Indolyl-3-ethanone-α-thioethers: a promising new class of non-toxic antimalarial agents
- Creator
- Svogie, Archibald L
- Creator
- Isaacs, Michelle
- Creator
- Hoppe, Heinrich C
- Creator
- Khanye, Setshaba D
- Creator
- Veale, Clinton G L
- Date Issued
- 2016
- Date
- 2016
- Type
- text
- Type
- article
- Identifier
- http://hdl.handle.net/10962/66233
- Identifier
- vital:28920
- Identifier
- https://doi.org/10.1016/j.ejmech.2016.02.056
- Description
- publisher version
- Description
- The success of chemotherapeutics in easing the burden of malaria is under continuous threat from ever-evolving parasite resistance, including resistance to artemisinin combination therapies. Therefore, the discovery of new classes of antimalarials which inhibit new biological targets is imperative to controlling malaria. Accordingly, we report here the discovery of indolyl-3-ethanone-α-thioethers, a new class of antimalarial compounds with encouraging activity. Synthesis of a focused library of compounds revealed important insight into the SAR of this class of compounds, including critical information regarding the position and chemical nature of substituents on both the thiophenol and indole rings. This investigation ultimately led to the discovery of two hit compounds (16 and 27) which exhibited nano molar in vitro antimalarial activity coupled to no observable toxicity against a HeLa cell line.
- Format
- 10 pages
- Format
- Language
- English
- Relation
- European Journal of Medicinal Chemistry
- Relation
- Svogie, Archibald L.,Isaacs, Michelle, Hoppe, Heinrich C., Khanye, Setshaba D., Veale, Clinton G. L.(2016) Indolyl-3-ethanone-α-thioethers: A promising new class of non-toxic antimalarial agents. European Journal of Medicinal Chemistry, 114, p.79-88. SN: 0223-5234. https://doi.org/10.1016/j.ejmech.2016.02.056
- Relation
- European Journal of Medicinal Chemistry volume 114 number 79 88 May 2016 0223-5234
- Rights
- Elsevier B.V.
- Rights
- Use of this resource is governed by the terms and conditions of the European Journal of Medicinal Chemistry Guide for Authors Open Access Statement (https://www.elsevier.com/journals/european-journal-of-medicinal-chemistry/0223-5234/guide-for-authors)
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Collections
Veale, Clinton G L (Dr)
Isaacs, Michelle (Mrs)
Hoppe, Heinrich C (Prof)
Khanye, David Setshaba (Associate Prof)
RU Department of Chemistry
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