Abstract
Two BODIPY-labeled colchicine derivatives were synthesized and shown to bind to tubulin but only partially inhibit tubulin polymerization in the presence of GTP. Cytotoxicity studies were carried out in HeLa, HepG2, Raji and Vero cells. Apoptosis-inducing properties were determined by caspase 3/7 activity and flow cytometry and interactions between the derivatives and tubulin were verified by fluorescence microscopy of living cells.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Boron Compounds / chemical synthesis*
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Boron Compounds / chemistry
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Cell Survival / drug effects
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Chlorocebus aethiops
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Colchicine / analogs & derivatives*
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Colchicine / chemistry*
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Colchicine / pharmacology
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Drug Screening Assays, Antitumor
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HeLa Cells
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Humans
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Hydrogen-Ion Concentration
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Microscopy, Fluorescence
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Microtubules / drug effects
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Molecular Structure
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Tubulin Modulators / chemistry*
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Tubulin Modulators / pharmacology
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Vero Cells
Substances
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4,4-difluoro-4-bora-3a,4a-diaza-s-indacene
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Boron Compounds
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Tubulin Modulators
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Colchicine