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Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection.
Asquith, Christopher R M; Sil, Bruno C; Laitinen, Tuomo; Tizzard, Graham J; Coles, Simon J; Poso, Antti; Hofmann-Lehmann, Regina; Hilton, Stephen T.
Afiliación
  • Asquith CRM; School of Pharmacy, Faculty of Life Sciences, University College London, London WC1N 1AX, United Kingdom; Clinical Laboratory & Center for Clinical Studies, Vetsuisse Faculty, University of Zurich, 8057 Zurich, Switzerland; Department of Pharmacology, School of Medicine, University of North Caro
  • Sil BC; School of Pharmacy, Faculty of Life Sciences, University College London, London WC1N 1AX, United Kingdom; School of Human Sciences, London Metropolitan University, 166-220 Holloway Road, London N7 8DB, United Kingdom.
  • Laitinen T; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, Kuopio 70211, Finland.
  • Tizzard GJ; UK National Crystallography Service, School of Chemistry, University of Southampton, Highfield Campus, Southampton SO17 1BJ, United Kingdom.
  • Coles SJ; UK National Crystallography Service, School of Chemistry, University of Southampton, Highfield Campus, Southampton SO17 1BJ, United Kingdom.
  • Poso A; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, Kuopio 70211, Finland.
  • Hofmann-Lehmann R; Clinical Laboratory & Center for Clinical Studies, Vetsuisse Faculty, University of Zurich, 8057 Zurich, Switzerland.
  • Hilton ST; School of Pharmacy, Faculty of Life Sciences, University College London, London WC1N 1AX, United Kingdom. Electronic address: s.hilton@ucl.ac.uk.
Bioorg Med Chem ; 27(18): 4174-4184, 2019 09 15.
Article en En | MEDLINE | ID: mdl-31395510
ABSTRACT
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.
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Piperazinas / Infecciones por VIH / Virus de la Inmunodeficiencia Felina / Proteínas de la Nucleocápside Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2019 Tipo del documento: Article
Texto completo
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Piperazinas / Infecciones por VIH / Virus de la Inmunodeficiencia Felina / Proteínas de la Nucleocápside Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2019 Tipo del documento: Article