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Sinteza derivatov 2-(4-okso-3-fenilizoksazolo[5,4-d]pirimidin-5(4H)-il)-N-fenilacetamida iz različno substituiranih aldehidov in anilinov kot zaviralcev indolamin 2,3-dioksigenaze 1 = The synthesis of 2-(4-oxo-3-phenylisoxazolo[5,4-d]pyrimidin-5(4H)-yl)-N-phenylacetamide derivatives from substituted aldehydes and anilines as indoleamine 2,3-dioxygenase 1 inhibitors : magistrska naloga : magistrski študijski program Industrijska farmacijaBombek, DomenZ imunoterapijo raka želimo ponovno vzpostaviti ravnovesje imunskega sistema, katerega delovanje rakaste celice s procesom imunskega preurejanja uporabijo za izboljšanje preživetja in pospešeno rast ... tumorja. Povečano izražanje inhibitornih receptorjev imenovanih kontrolne točke, ki v organizmu skrbijo za periferno toleranco in nadzorujejo jakost imunskega odziva, je eden izmed mehanizmov, kjer tumorske celice izkoristijo imunski sistem za zagotovitev imunskega pobega. Indolamin 2,3-dioksigenaza 1 (IDO1) je znotrajcelična hemvsebujoča oksidoreduktaza, ki sodeluje pri kinureninski poti razgradnje triptofana do kinurenina ter ostalih metabolitov. Znižana koncentracija triptofana in povišana koncentracija kinurenina in ostalih metabolitov v organizmu sproži zaviranje imunskega odziva in širjenje tumorja. IDO1 zato predstavlja ustrezno tarčo za iskanje novih protirakavih učinkovin, ki v organizmu ponovno vzpostavijo imunsko ravnovesje. V sklopu magistrske naloge smo želeli sintetizirati nove potencialne zaviralce IDO1 na osnovi strukture 2-(4-okso-3-fenilizoksazolo[5,4-d]pirimidin-5(4H)-il)-N-fenilacetamida. Osnovna sintezna pot do končnih produktov je obsegala pet stopenj, alkilante za reakcijo N-alkiliranja pa smo pripravili z enostopenjsko sintezo. Intermediatom in končnim produktom smo z različnimi analitskimi metodami določili njihove fizikalno-kemijske lastnosti in potrdili njihovo istovetnost in čistost. Končnim spojinam smo z uporabo biokemijskega testiranja na osnovi spremljanja fluorescence ovrednotili njihovo zaviralno aktivnost na IDO1. Vsi pridobljeni produkti, razen N-(4-nitrofenil)-2-(4-okso-3-(p-tolil)izoksazolo[5,4-d]pirimidin-5(4H)-ilacetamida (14), so se izkazali za slabe zaviralce encima. Slednji je izkazal 45 % zaviranje pri 100 μM, zaradi česar je bil edini ustrezen produkt, ki mu je bilo smiselno določiti vrednost IC50, ki je znašala 145 μM. Uspelo nam je torej sintetizirati en zaviralec IDO1 z aktivnostjo v mikromolarnem območju, hkrati pa smo pridobili nove podatke o vplivu substitucij na fenilnem obroču vezanim na izoksazolno in acetamidno skupino, ki jih bomo lahko uporabili za nadaljnje delo pri razvoju novih zaviralcev encima IDO1.Type of material - master's thesis ; adult, seriousPublication and manufacture - Ljubljana : [D. Bombek], 2022Language - slovenianCOBISS.SI-ID - 109051651
Author
Bombek, Domen
Other authors
Sova, Matej, 1979-
Topics
Rak (medicina) |
Imunoterapija |
indolamin 2, 3-dioksigenaza 1 |
zaviralci IDO1 |
kinureninska pot |
imunsko preurejanje |
sinteze benzaldehid oksima
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Library/institution |
City | Acronym | For loan | Other holdings |
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Faculty of Pharmacy, Ljubljana | Ljubljana | FFALJ |
reading room 1 cop.
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Bombek, Domen | ![]() |
Sova, Matej, 1979- | 25490 |
Source: Personal bibliographies
and: SICRIS
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