Sebastian Demkowicz - Publications - Bridge of Knowledge

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  • An efficient and convenient synthesis of unsymmetrical disulfides from thioacetates
    Publication

    We have developed convenient methods for the synthesis of functionalized unsymmetrical dialkyl disulfides under mild conditions in very good yields. The designed method is based on the reaction of (5,5-dimethyl-2-thioxo-1,3,2-dioxaphosphorinan-2-yl)-disulfanyl derivatives 1 with functionalized alkyl thiolate anions, generated in situ from thioacetates2and sodium methoxide or butylamine. The developed method allows the preparation...

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  • New clicked full agonists of the estrogen receptor β
    Publication
    • S. Demkowicz
    • K. Filipiak
    • M. Maslyk
    • J. Ciepielski
    • S. de Pascual-Teresa
    • S. Martín-Santamaría
    • B. De Pascual-Teresa
    • A. Ramos

    - RSC Advances - Year 2013

    A click chemistry approach was used to synthesize a series of 1,4-diaryl-substituted 1,2,3-triazoles designed to behave as estrogen receptor (ER) ligands. We studied their affinities for both receptors α and β, their agonist activities in a cell-based luciferase reporter assay and their effect on the proliferation of the hormone-dependent MCF-7 cell line. We found two compounds (3a and 3c) that behave as selective full agonists...

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Year 2012
  • Towards β-selectivity in functional estrogen receptor antagonists
    Publication
    • J. J. Rodríguez
    • K. Filipiak
    • M. Maslyk
    • J. Ciepielski
    • S. Demkowicz
    • S. de Pascual-Teresa
    • S. Martín-Santamaría
    • B. d. P. ..
    • A. Ramos

    - ORGANIC & BIOMOLECULAR CHEMISTRY - Year 2012

    Based on the benzo[b]naphtho[1,2-d]furan and benzo[b]naphtho[1,2-d]thiophene frameworks, a series of ligands with different basic side chains (BSCs) has been synthesized and pharmacologically evaluated. Also, their binding modes have been modelled using docking techniques. It was found that the introduction of a BSC in these systems brings about a decrease of affinity for both estrogen receptors α and β in an in vitro competitive...

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