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

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.

journal_name

Bioorg Med Chem

authors

Asquith CRM,Sil BC,Laitinen T,Tizzard GJ,Coles SJ,Poso A,Hofmann-Lehmann R,Hilton ST

doi

10.1016/j.bmc.2019.07.047

subject

Has Abstract

pub_date

2019-09-15 00:00:00

pages

4174-4184

issue

18

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(19)31030-2

journal_volume

27

pub_type

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