Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 19, Issue 17, Pages 5247-5254Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.06.082
Keywords
Discodermolide; Tubulin; Synthesis; Fluorescence
Funding
- NIH [CA-69571]
- NSF [CHE-0619382]
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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 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. (C) 2011 Elsevier Ltd. All rights reserved.
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