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  • Synthesis of thicolchicine - based conjugates [Elektronski vir] : investigation towards bivalent tubulin/microtubules binders
    Bonandi, Elisa ...
    Four different hybrid compounds have been efficiently synthesized by conjugation of deacetylthiocolchicine with pironetin-inspired derivatives. The modest bioactivity and the apparent absence of ... interaction with [alpha] - tubulin is explained by a posteriori in silico investigation, which suggests a relevant distance between the thiocolchicine binding site and the proper pocket on the [alpha]-tubulin. The modest activity on resistant cells suggested that the lipophilic nature of the linker used renders the resulting compounds better substrates for p-Gp efflux pumps. The study better clarifies the design of bivalent compounds that target hetero tubulin/microtubules.
    Source: ChemPlusChem [Elektronski vir]. - ISSN 2192-6506 (Vol. 84, iss. 1, Jan. 2019, str. 98-102)
    Type of material - e-article
    Publish date - 2019
    Language - english
    COBISS.SI-ID - 4657777

    Link(s):

    https://onlinelibrary.wiley.com/doi/10.1002/cplu.201800497
    DOI

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