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Asquith, Christopher R. M., Sil dos Santos, Bruno, Laitinen, Tuomo, Tizzard, Graham J., Coles, Simon J., Poso, Antti, Hofmann-Lehmann, Regina and 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). pp. 4174-4184. ISSN 0968-0896
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.
Available under License Creative Commons Attribution Non-commercial No Derivatives 4.0.
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