Abstract
A Prins cyclization between a polymer-bound aldehyde and a homoallylic alcohol served as the key step in the synthesis of tetrahydropyran derivatives. A phenotypic screen led to the identification of compounds that inhibit mitosis (as seen by the accumulation of round cells with condensed DNA and membrane blebs). These compounds were termed tubulexins as they target the CSE1L protein and the vinca alkaloid binding site of tubulin.
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Binding Sites
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Cellular Apoptosis Susceptibility Protein / chemistry
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Cellular Apoptosis Susceptibility Protein / metabolism*
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HeLa Cells
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Humans
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MCF-7 Cells
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Mitosis / drug effects
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Mitosis Modulators
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Pyrans / chemical synthesis*
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Pyrans / chemistry
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Pyrans / pharmacology*
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Tubulin / chemistry
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Tubulin / metabolism*
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Tubulin Modulators / chemical synthesis
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Tubulin Modulators / chemistry
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Tubulin Modulators / pharmacology
Substances
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Cellular Apoptosis Susceptibility Protein
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Mitosis Modulators
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Pyrans
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Tubulin
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Tubulin Modulators