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Sinteza analogov 2-(3-(4-fluorofenil)-4-oksoizoksazolo[5,4-d]pirimidin-5(4H)-il)-N-fenilacetamida kot zaviralcev indolamin 2,3-dioksigenaze 1 = Synthesis of 2-(3-(4-fluorophenyl)-4-oxoisoxazolo[5,4-d]pyrimidin-5(4H)-yl)-N-phenylacetamide analogs as indoleamine 2,3-dioxygenase 1 inhibitors : magistrski študijski program Industrijska farmacijaKožuh, EvaČloveški imunski sistem je kompleksen sistem različnih celic, tkiv in organov. Zadolžen je za odgovor na različne notranje ali zunanje grožnje, ena izmed njih predstavlja razvoj rakavih celic. Na ... transformacijo normalnih celic v rakave lahko vpliva več dejavnikov, tako zunanjih kot notranjih, pomembno vlogo pri širjenju raka pa ima tudi znotrajcelični citosolni encim indolamin 2,3-dioksigenaza 1 (IDO1), ki sodeluje v kinureninski razgradni poti (KP) esencialne aminokisline triptofan (Trp). Ekspresija IDO1 v celicah tako vpliva na razmerje med koncentracijo Trp in metabolitov KP, ki imajo imunosupresivno delovanje in zavirajo odziv imunskega sistema na rakave celice. Število na novo odkritih zaviralcev IDO1 se povečuje, saj velika farmacevtska podjetja vlagajo v njihov razvoj, veliko od njih se jih je znašlo že v kliničnih raziskavah. V okviru magistrske naloge smo sintetizirali pet končnih spojin, ki smo jim ovrednotili zaviralno delovanje na IDO1. Vseh pet spojin ima enak skelet, ki temelji na zadetku iz virtualnega rešetanja 3-(4-fluorofenil)izooksazolo[5,4-d]pirimidin- 4(5H)-onu. Spojine smo analitsko ovrednotili in zaviralno aktivnost preverili s pomočjo biokemijskega testiranja na osnovi merjenja fluorescence. Od sintetiziranih spojin, ki se med seboj razlikujejo v substituciji na fenilnem obroču, sta le dve izkazovali signifikantno zaviralno delovanje. Spojinam 12 in 13 smo določili in izračunali vrednost IC50 v nizkem mikromolarnem območju, zato lahko sklepamo, da se cikloheksilni obroč ali trifluorometilna skupina, ki sta vezani na fenilacetamidni fragment, najbolje prilegata v žep B v aktivnem mestu encima IDO1, kar smo potrdili tudi z molekulskim sidranjem spojine 12 v kristalno strukturo encima IDO1. Z ustrezno optimizacijo predstavlja spojina 12 dobro izhodišče za razvoj močnega zaviralca encima IDO1, ki bi ga lahko v prihodnosti uporabljali kot protitumorno učinkovino.Type of material - master's thesis ; adult, seriousPublication and manufacture - Ljubljana : [E. Kožuh], 2020Language - slovenianCOBISS.SI-ID - 28251651
Author
Kožuh, Eva
Other authors
Sova, Matej, 1979-
Topics
Rak (medicina) |
Imunski sistem |
indolamin 2, 3-dioksigenaza 1 (IDO1) |
zaviralci |
kinureninska razgradna pot |
triptofan
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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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Kožuh, Eva | ![]() |
Sova, Matej, 1979- | 25490 |
Source: Personal bibliographies
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