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 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

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Abstract / Description

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:	Article
Uncontrolled Keywords:	Epidithiodiketopiperazines (ETP)Zinc ejectionFeline Immunodeficiency Virus (FIV)Human Immunodeficiency Virus (HIV)Nucleocapsid protein (NCp)
Subjects:	500 Natural Sciences and Mathematics > 540 Chemistry & allied sciences 600 Technology > 610 Medicine & health
Department:	School of Human Sciences
Depositing User:	Bruno Da Silva sil dos santos
Date Deposited:	10 Oct 2019 10:53
Last Modified:	14 Sep 2020 14:06
URI:	https://repository.londonmet.ac.uk/id/eprint/5054

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