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 Chemjournal_title
Bioorganic & medicinal chemistryauthors
Asquith CRM,Sil BC,Laitinen T,Tizzard GJ,Coles SJ,Poso A,Hofmann-Lehmann R,Hilton STdoi
10.1016/j.bmc.2019.07.047subject
Has Abstractpub_date
2019-09-15 00:00:00pages
4174-4184issue
18eissn
0968-0896issn
1464-3391pii
S0968-0896(19)31030-2journal_volume
27pub_type
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