Spelling suggestions: "subject:"dibenz[c,e]oxepin"" "subject:"dibenz[c,e]oxepane""
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Tubulin-binding dibenz[c,e]oxepines. Part 2. 1 Structural variation and biological evaluation as tumour vasculature disrupting agentsRossington, S.B., Hadfield, J.A., Shnyder, Steven, Wallace, T.W., Williams, K.J. 19 January 2017 (has links)
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.
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