2. Academic Validation
  3. A 2-step synthesis of Combretastatin A-4 and derivatives as potent tubulin assembly inhibitors

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

  • Bioorg Med Chem. 2020 Oct 1;28(19):115684. doi: 10.1016/j.bmc.2020.115684.
Natalie G Barnes 1,  Anthony W Parker 2,  Amjed A Ahmed Mal Ullah 1,  Patricia A Ragazzon 1,  John A Hadfield 3
Affiliations

Affiliations

  • 1 Biomedical Research Centre, Kidscan Laboratories, School of Science, Engineering and Environment, University of Salford, Salford, UK.
  • 2 Central Laser Facility, Research Complex at Harwell, Rutherford Appleton Laboratory, STFC, Chilton, Oxfordshire OX11 0QX, UK.
  • 3 Biomedical Research Centre, Kidscan Laboratories, School of Science, Engineering and Environment, University of Salford, Salford, UK. Electronic address: j.a.hadfield@salford.ac.uk.
PMID: 32912434 DOI: 10.1016/j.bmc.2020.115684
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.

Keywords

Cancer; Combretastatin A-4; Microtubules; Tubulin.

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