A 2-step synthesis of Combretastatin A-4 and derivatives as potent tubulin assembly inhibitors

Barnes, N, Parker, AW, Mal Ullah, AA, Ragazzon, PA and Hadfield, JA ORCID: https://orcid.org/0000-0001-7984-8319 2020, 'A 2-step synthesis of Combretastatin A-4 and derivatives as potent tubulin assembly inhibitors' , Bioorganic and Medicinal Chemistry, 28 (19) , p. 115684.

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A series of combretastatin derivatives were designed and synthesised by a two-step stereoselective synthesis by use of Wittig olefination followed by Suzuki cross-coupling. Interestingly, all new compounds (2a-2i) showed potent cell-based antiproliferative activities in nanomolar concentrations. Among the compounds, 2a, 2b and 2e were the most active across three cancer cell lines. In addition, these compounds inhibited the polymerisation of tubulin in vitro more efficiently than CA-4. They caused cell cycle arrest in G2/M phase further confirming their ability to inhibit tubulin polymerisation.

Item Type: Article
Schools: Schools > School of Environment and Life Sciences > Biomedical Research Centre
Journal or Publication Title: Bioorganic and Medicinal Chemistry
Publisher: Elsevier
ISSN: 0968-0896
Related URLs:
Funders: Kidscan, Engineering and Physical Sciences Research Council (EPSRC)
Depositing User: JA Hadfield
Date Deposited: 20 Aug 2020 10:35
Last Modified: 16 Feb 2022 05:23
URI: http://usir.salford.ac.uk/id/eprint/57981

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