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

Design, synthesis and biological evaluation of a simplified fluorescently labeled discodermolide (cas 127943-53-7) as a molecular probe to study the binding of discodermolide (cas 127943-53-7) to tubulin
Add time:08/20/2019 Source:sciencedirect.com

The design, synthesis, and biological evaluation of a simplified fluorescently labeled discodermolide (cas 127943-53-7) 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 molecular probe to explore the local environment of the discodermolide binding site on tubulin. The results of fluorescence measurements on the tubulin-bound analogue are reported.

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