Abstract
Three fluorescent probes 3a,3b, and 4 have been synthesized through conjugation of fluorescein and difluorescein groups to the 7-OH of C-2 modified paclitaxel and cephalomannine derivatives with very high affinity to microtubules. All these probes exhibited potent tubulin assembly promotion and tumor cell killing activities, thus may be useful as tools for the determination of thermodynamic parameters and exploration of ligand-microtubule interactions.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anisotropy
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Bridged-Ring Compounds / chemistry*
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Chemistry, Pharmaceutical / methods*
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Dose-Response Relationship, Drug
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Drug Design
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Fluorescein / chemistry
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Fluorescent Dyes / chemical synthesis*
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Fluorescent Dyes / pharmacology*
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Ligands
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Microtubules / metabolism
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Models, Chemical
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Plant Extracts / metabolism
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Taxoids / chemical synthesis
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Taxoids / chemistry*
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Temperature
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Thermodynamics
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Tubulin / chemistry
Substances
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Bridged-Ring Compounds
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Fluorescent Dyes
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Ligands
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Plant Extracts
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Taxoids
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Tubulin
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taxane
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cephalomannine
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Fluorescein