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Synthesis and Biological Evaluation of Colchicine B‑Ring Analogues Tethered with Halogenated Benzyl Moieties

AuthorsCosentino, Laura; Redondo-Horcajo, Mariano ; Zhao, Ying; Santos, Ana Rita; Chowdury, Kaniz F.; Vinader, Victoria; Abdallah, Qasem M. A.; Abdel-Rahman, Hamdy; Fournier-Dit-Chabert, Jérémie; Shnyder, Steven D.; Loadman, Paul M.; Fang, Wei-shuo S.; Díaz, José Fernando ; Barasoain, Isabel ; Burns, Philip A.; Pors, Klaus
Issue Date2012
PublisherAmerican Chemical Society
CitationJournal of Medicinal Chemistry, 55 (24) : 11062-11066 (2012)
AbstractDeacetylcolchicine was reacted with substituted benzyl halides to provide a library of compounds for biological analysis. Compound 7 (3,4-difluorobenzyl-N-aminocolchicine) was shown to possess cytotoxicity in cancer cell lines in the low nanomolar range. Significantly, it showed no loss of activity in the resistant A2780AD ovarian carcinoma cell line known to overexpress the ABCB1 drug transporter and was also unaffected by overexpression of class III β-tubulin in HeLa transfected cells
Description5 páginas, 3 figuras, 3 tablas, 1 esquema -- PAGS nros. 11062-11066
Publisher version (URL)http://dx.doi.org/10.1021/jm301151t
Appears in Collections:(CIB) Artículos
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