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Asquith, Christopher R M; Sil, Bruno C; Laitinen, Tuomo; Tizzard, Graham J; Coles, Simon J; Poso, Antti; Hofmann-Lehmann, Regina; Hilton, Stephen T (2019). Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection. Bioorganic & Medicinal Chemistry, 27(18):4174-4184.
Focused libraries of multi-substituted epidithiodiketopiperazines (ETP) were prepared and evaluated for efficacy of inhibiting the nucleocapsid protein function of the Feline Immunodeficiency Virus (FIV) as a model for HIV. This activity was compared and contrasted to observed toxicity utilising an in-vitro cell culture approach. This resulted in the identification of several promising lead compounds with nanomolar potency in cells with low toxicity and a favorable therapeutic index.
| Item Type: | Journal Article, refereed, original work |
|---|---|
| Communities & Collections: | 05 Vetsuisse Faculty > Veterinary Clinic > Department of Clinical Diagnostics and Services
05 Vetsuisse Faculty > Center for Clinical Studies |
| Dewey Decimal Classification: | 610 Medicine & health |
| Scopus Subject Areas: | Life Sciences > Biochemistry
Life Sciences > Molecular Medicine Life Sciences > Molecular Biology Life Sciences > Pharmaceutical Science Life Sciences > Drug Discovery Life Sciences > Clinical Biochemistry Physical Sciences > Organic Chemistry |
| Uncontrolled Keywords: | Epidithiodiketopiperazines (ETP); Feline Immunodeficiency Virus (FIV); Human Immunodeficiency Virus (HIV); Nucleocapsid protein (NCp); Zinc ejection |
| Language: | English |
| Date: | 15 September 2019 |
| Deposited On: | 22 Jan 2020 15:43 |
| Last Modified: | 22 Mar 2025 02:35 |
| Publisher: | Elsevier |
| ISSN: | 0968-0896 |
| OA Status: | Closed |
| Publisher DOI: | https://doi.org/10.1016/j.bmc.2019.07.047 |
| PubMed ID: | 31395510 |
Asquith, Christopher R M