Hadfield, JA 
ORCID: https://orcid.org/0000-0001-7984-8319, Rossington, SB, Wallace, TW, Shnyder, SD and Williams, KJ
2017,
'Tubulin-binding dibenz[c,e]oxepines: Part 2 Structural variation and biological evaluation as tumour vasculature disrupting agents'
, Bioorganic and Medicinal Chemistry, 25 (5)
, pp. 1630-1642.
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Abstract
5,7-Dihydro-3,9,10,11-tetramethoxybenz[c,e]oxepin-4-ol 1, prepared from a dibenzyl ether precursor via Pd-catalysed intramolecular direct arylation, possesses broad-spectrum in vitro cytotoxicity towards various tumour cell lines, and induces vascular shutdown, necrosis and growth delay in tumour xenografts in mice at sub-toxic doses. The biological properties of 1 and related compounds can be attributed to their ability to inhibit microtubule assembly at the micromolar level, by binding reversibly to the same site of the tubulin αβ-heterodimer as colchicine 2 and the allocolchinol, N-acetylcolchinol 4.
| 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: | UMIP |
| Depositing User: | JA Hadfield |
| Date Deposited: | 30 Jan 2017 09:55 |
| Last Modified: | 15 Feb 2022 21:39 |
| URI: | https://usir.salford.ac.uk/id/eprint/41266 |
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