Design, synthesis and biological evaluation of a simplified fluorescently labeled discodermolide as a molecular probe to study the binding of discodermolide to tubulin

J Qi, AR Blanden, S Bane, DGI Kingston

Index: Qi, Jun; Blanden, Adam R.; Bane, Susan; Kingston, David G.I. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 17 p. 5247 - 5254

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Citation Number: 5

Abstract

Abstract The design, synthesis, and biological evaluation of a simplified fluorescently labeled discodermolide analogue possessing a dimethylaminobenzoyl fluorophore has been achieved. Stereoselective Suzuki coupling and Horner–Wadsworth–Emmons reaction comprised the key tactics for its construction. The analogue exhibited qualitatively similar activity to paclitaxel in a tubulin assembly assay, and it can thus be used as a fluorescent ...