Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection
Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection
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.
Epidithiodiketopiperazines (ETP), Zinc ejection, Feline Immunodeficiency Virus (FIV), Human Immunodeficiency Virus (HIV), Nucleocapsid protein (NCp)
4174-4184
Asquith, Christopher R.M.
c00d3c3f-08c5-4c9a-bac8-0fc485db1be4
Sil, Bruno C.
83be81f1-53b4-4af9-bdfa-9e8f8b1f66ea
Laitinen, Tuomo
b37037c5-4eac-4533-8246-5a49213bae9b
Tizzard, Graham J.
8474c0fa-40df-43a6-a662-7f3c4722dbf2
Coles, Simon J.
3116f58b-c30c-48cf-bdd5-397d1c1fecf8
Poso, Antii
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Hofmann-Lehmann, Regina
0c1c2056-848e-469c-8bb9-0258293160de
Hilton, Stephen T.
b3c15d45-c69d-47cd-a367-77a43e3fdbed
15 September 2019
Asquith, Christopher R.M.
c00d3c3f-08c5-4c9a-bac8-0fc485db1be4
Sil, Bruno C.
83be81f1-53b4-4af9-bdfa-9e8f8b1f66ea
Laitinen, Tuomo
b37037c5-4eac-4533-8246-5a49213bae9b
Tizzard, Graham J.
8474c0fa-40df-43a6-a662-7f3c4722dbf2
Coles, Simon J.
3116f58b-c30c-48cf-bdd5-397d1c1fecf8
Poso, Antii
4563f55e-93b3-4df8-a5a6-1e75a4cd8455
Hofmann-Lehmann, Regina
0c1c2056-848e-469c-8bb9-0258293160de
Hilton, Stephen T.
b3c15d45-c69d-47cd-a367-77a43e3fdbed
Asquith, Christopher R.M., Sil, Bruno C., Laitinen, Tuomo, Tizzard, Graham J., Coles, Simon J., Poso, Antii, 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), .
(doi:10.1016/j.bmc.2019.07.047).
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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Accepted/In Press date: 28 July 2019
e-pub ahead of print date: 30 July 2019
Published date: 15 September 2019
Keywords:
Epidithiodiketopiperazines (ETP), Zinc ejection, Feline Immunodeficiency Virus (FIV), Human Immunodeficiency Virus (HIV), Nucleocapsid protein (NCp)
Identifiers
Local EPrints ID: 434438
URI: http://eprints.soton.ac.uk/id/eprint/434438
ISSN: 0968-0896
PURE UUID: 24a7c04b-5c23-4878-b98e-7d5182c27295
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Date deposited: 23 Sep 2019 16:31
Last modified: 17 Mar 2024 02:53
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Contributors
Author:
Christopher R.M. Asquith
Author:
Bruno C. Sil
Author:
Tuomo Laitinen
Author:
Antii Poso
Author:
Regina Hofmann-Lehmann
Author:
Stephen T. Hilton
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