Tubulin-binding dibenz[c,e]oxepines as colchinol analogues for targeting tumour vasculature.
Posted by rob on November 18, 2010 under Uncategorized | 
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Tubulin-binding dibenz[c,e]oxepines as colchinol analogues for targeting tumour vasculature.
Org Biomol Chem. 2010 Nov 17;
Authors: Edwards DJ, Hadfield JA, Wallace TW, Ducki S
Various methoxy- and hydroxy-substituted dibenz[c,e]oxepines were prepared via the copper(i)-induced coupling of ether-tethered arylstannanes or the dehydrative cyclisation of 1,1′-biphenyl-2,2′-dimethanols, assembled using the Ullmann cross-coupling of ortho-bromoaryl carbonyl compounds. The dibenzoxepines were screened for their ability to inhibit tubulin polymerisation and the in vitro growth of K562 human chronic myelogenous leukemia cells. The most active was 5,7-dihydro-3,9,10,11-tetramethoxydibenz[c,e]oxepin-4-ol, whose tubulin inhibitory and cytotoxicity (IC(50)) values were 1 ?M and 40 nM, respectively.
PMID: 21082139 [PubMed - as supplied by publisher]