Asquith, CRM;
Sil, BC;
Laitinen, T;
Tizzard, GJ;
Coles, SJ;
Poso, A;
Hofmann-Lehmann, R;
(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.
10.1016/j.bmc.2019.07.047.
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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.
| Type: | Article |
|---|---|
| Title: | Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection |
| Location: | England |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1016/j.bmc.2019.07.047 |
| Publisher version: | https://doi.org/10.1016/j.bmc.2019.07.047 |
| Language: | English |
| Additional information: | This version is the author accepted manuscript. For information on re-use, please refer to the publisher’s terms and conditions. |
| Keywords: | Epidithiodiketopiperazines (ETP), Zinc ejection, Feline Immunodeficiency Virus (FIV), Human Immunodeficiency Virus (HIV), Nucleocapsid protein (NCp) |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharma and Bio Chemistry |
| URI: | https://discovery.ucl.ac.uk/id/eprint/10082926 |
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