Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection

Bioorganic & Medicinal Chemistry
Christopher R M AsquithStephen T Hilton

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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Citations

Jun 25, 2021·Chemical Science·Yangyang ChengStefan Matile
Jul 24, 2020·Journal of the American Chemical Society·Henry R KilgoreRonald T Raines
Mar 4, 2020·The Journal of Organic Chemistry·Chase R OlssonMohammad Movassaghi

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