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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

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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

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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Title:
Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection
Creators:
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.
Identification Number:
https://doi.org/10.1016/j.bmc.2019.07.047
Date:
15 September 2019
Subjects:
500 Natural Sciences and Mathematics > 540 Chemistry & allied sciences
600 Technology > 610 Medicine & health
Department:
School of Human Sciences
Publisher:
Elsevier
Uncontrolled Keywords:
Epidithiodiketopiperazines (ETP)Zinc ejectionFeline Immunodeficiency Virus (FIV)Human Immunodeficiency Virus (HIV)Nucleocapsid protein (NCp)
Record
URI:
https://repository.londonmet.ac.uk/id/eprint/5054
Item Type:
Article
Depositing User:
Bruno Da Silva sil dos santos
Date Deposited:
10 Oct 2019 10:53
Revision:
30
Last Modified:
14 Sep 2020 14:06
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