Yes / 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.
Identifer | oai:union.ndltd.org:BRADFORD/oai:bradscholars.brad.ac.uk:10454/11235 |
Date | 19 January 2017 |
Creators | Rossington, S.B., Hadfield, J.A., Shnyder, Steven, Wallace, T.W., Williams, K.J. |
Source Sets | Bradford Scholars |
Language | English |
Detected Language | English |
Type | Article, Accepted manuscript |
Rights | © 2017 Elsevier. Reproduced in accordance with the publisher's selfarchiving policy. This manuscript version is made available under the CC-BY-NC-ND 4.0 license (http://creativecommons.org/licenses/by-nc-nd/4.0/), CC-BY-NC-ND |
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