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SYNTHESIS AND EVALUATION OF ACETYL DERIVATIVES OF DIBENZOCYCLOOCTADIENE LIGNANS AS P-GLYCOPROTEIN INHIBITORS

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216224%3A14110%2F19%3A00110717" target="_blank" >RIV/00216224:14110/19:00110717 - isvavai.cz</a>

  • Result on the web

    <a href="http://www.skolams.cz/" target="_blank" >http://www.skolams.cz/</a>

  • DOI - Digital Object Identifier

Alternative languages

  • Result language

    angličtina

  • Original language name

    SYNTHESIS AND EVALUATION OF ACETYL DERIVATIVES OF DIBENZOCYCLOOCTADIENE LIGNANS AS P-GLYCOPROTEIN INHIBITORS

  • Original language description

    P-glycoprotein is typical ATP binding cassette (ABC) transporter responsible for the transportation out of cells of various xenobiotics including cytostatic compounds. A possible method for overcoming the resistance to anticancer drugs is the coadministration of compounds showing low toxicity and an ability to inhibit ABC transporters. Promising inhibitory activity has been discovered group of plant phenols, the dibenzocyclooctadiene lignans, from two plant genera Schisandra and Kadsura. The main source of these lignans are the fruits of Schisandra chinensis. In previous works three main structural features of dibenzocyclooctadiene lignans involved in P-glycoprotein inhibition were revealed: a 1,2,3-trimethoxy moiety, a 6- acyloxy group, and the absence of a 7-hydroxy group. To prepare more active derivatives, 7-hydroxy group was modified by acetylation.

  • Czech name

  • Czech description

Classification

  • Type

    O - Miscellaneous

  • CEP classification

  • OECD FORD branch

    30104 - Pharmacology and pharmacy

Result continuities

  • Project

  • Continuities

    S - Specificky vyzkum na vysokych skolach

Others

  • Publication year

    2019

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů