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Sinteza analogov deksrazoksana kot zaviralcev človeške DNA-topoizomeraze II
ID Anđelković, Marija (Author), ID Zidar, Nace (Mentor) More about this mentor... This link opens in a new window

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Abstract
V sklopu magistrske naloge smo sintetizirali in ovrednotili nekaj novih analogov deksrazoksana, kot potencialnih zaviralcev človeške DNA-topoizomeraze II. Pri večini načrtovanih spojin smo strukturne spremembe želeli uvesti na osrednji propan-1,2-diilni fragment, ki v molekuli deksrazoksana povezuje dva piperazin-2,6-dionska heterocikla. Pripraviti smo želeli dve spojini, ki imata na osrednjem delu namesto metilne skupine vezano pentilno skupino ali fenilni obroč, vendar žal zadnja stopnja sinteze ni bila uspešna. Uspešno pa smo pripravili spojino 11, ki ima namesto obeh piperazin-2,6-dionskih heterociklov vezana piperazin-2-onska obroča, ki sta povezana z 1-oksoetan-1,2-diilnim povezovalcem. Vse nove spojine smo fizikalno-kemijsko ovrednotili, s čemer smo potrdili njihovo identiteto in čistost.

Language:Slovenian
Keywords:deksrazoksan, DNA-topoizomeraza II, protirakava učinkovina, zaviralec
Work type:Master's thesis/paper
Organization:FFA - Faculty of Pharmacy
Year:2023
PID:20.500.12556/RUL-147025 This link opens in a new window
Publication date in RUL:21.06.2023
Views:1014
Downloads:60
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Secondary language

Language:English
Title:Synthesis of dexrazoxane analogues as human DNA topoisomerase II inhibitors
Abstract:
In our master's thesis, we synthesised and evaluated some new dexrazoxane analogues as potential inhibitors of human DNA topoisomerase II. For most of the proposed compounds, we wanted to make structural changes to the central propane-1,2-diyl that links the two piperazine-2,6-dione heterocycles in the dexrazoxane molecule. We wanted to prepare two compounds that have a pentyl group or a phenyl ring in the central part instead of a methyl group, but unfortunately the last step of the synthesis was not successful. However, we successfully prepared compound 11 containing piperazine-2,6-dione heterocycles instead of the two piperazine-2,6-dione heterocycles linked with a 1-oxoethane-1,2-diyl linker. We have physicochemically investigated all new compounds and confirmed their identity and purity.

Keywords:dexrazoxane, DNA-topoisomerase II, antitumor agent, inhibitor

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