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Barnes, N, Parker, A, Ahmed, A, Ragazzon, P and Hadfield, J (2020) A 2-step synthesis of Combretastatin A-4 and derivatives as potent tubulin assembly inhibitors. Bioorganic and Medicinal Chemistry, 28 (19). ISSN 1464-3391

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Abstract

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
Additional Information: The final accepted version of this article and all relevant information related to it can be found online at; https://www.sciencedirect.com/science/article/pii/S0968089620305149
Uncontrolled Keywords: Combretastatin A-4TubulinCancerMicrotubules
Subjects: Q Science > Q Science (General)
R Medicine > R Medicine (General)
R Medicine > R Medicine (General) > R735 Medical education. Medical schools. Research
R Medicine > RM Therapeutics. Pharmacology
Divisions: Faculty of Medicine and Health Sciences > School of Pharmacy and Bioengineering
Depositing User: Symplectic
Date Deposited: 06 Aug 2020 11:04
Last Modified: 05 Sep 2021 01:30
URI: https://eprints.keele.ac.uk/id/eprint/8473

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