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

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DRABINOVÁ Martina ČARNECKÁ Martina HUMPA Otakar SLANINOVÁ Iva SLANINA Jiří

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Fakulta / Pracoviště MU

Lékařská fakulta

Citace
Popis 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.
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