UCL Discovery
UCL home » Library Services » Electronic resources » UCL Discovery

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

Barnes, NG; Parker, AW; Ullah, AAAM; Ragazzon, PA; Hadfield, JA; (2020) A 2-step synthesis of Combretastatin A-4 and derivatives as potent tubulin assembly inhibitors. Bioorganic & Medicinal Chemistry , 28 (19) , Article 115684. 10.1016/j.bmc.2020.115684. Green open access

[thumbnail of BMCHEM-D-20-00677_.pdf]
Preview
Text
BMCHEM-D-20-00677_.pdf - Accepted Version

Download (533kB) | Preview

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.

Type: Article
Title: A 2-step synthesis of Combretastatin A-4 and derivatives as potent tubulin assembly inhibitors
Open access status: An open access version is available from UCL Discovery
DOI: 10.1016/j.bmc.2020.115684
Publisher version: https://doi.org/10.1016/j.bmc.2020.115684
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.
UCL classification: UCL
UCL > Provost and Vice Provost Offices > UCL BEAMS
UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences
UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences > Dept of Chemistry
URI: https://discovery.ucl.ac.uk/id/eprint/10114228
Downloads since deposit
53Downloads
Download activity - last month
Download activity - last 12 months
Downloads by country - last 12 months

Archive Staff Only

View Item View Item