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.
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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.
| 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 |
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