Abstract
Noscapine and its 7-hydroxy and 7-amino derivatives were characterized for their binding to tubulin. A solution NMR structure of these compounds bound to tubulin shows that noscapine and its 7-aniline derivative do not compete for the same binding site nor does its small molecule crystal structure match its tubulin-bound conformation. These compounds were also tested for their antiproliferative effects on a panel hepatocellular carcinoma cell lines.
MeSH terms
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Aniline Compounds / chemical synthesis*
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Aniline Compounds / pharmacology
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Binding Sites
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Cell Line, Tumor
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Cell Survival / drug effects
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Crystallography, X-Ray
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Drug Screening Assays, Antitumor
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Fluorescence
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Humans
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Magnetic Resonance Spectroscopy
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Molecular Conformation
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Noscapine / analogs & derivatives*
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Noscapine / chemical synthesis*
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Noscapine / pharmacology
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Protein Binding
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Solutions
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Structure-Activity Relationship
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Tubulin / chemistry*
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Tubulin Modulators / chemical synthesis*
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Tubulin Modulators / pharmacology
Substances
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Aniline Compounds
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Antineoplastic Agents
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Solutions
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Tubulin
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Tubulin Modulators
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Noscapine