Návrh a syntéza nových potenciálně cytotoxicky aktivních salicylamidů

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dc.contributor.author Dušek, Jan
dc.date.accessioned 2020-07-22T07:37:56Z
dc.date.available 2020-07-22T07:37:56Z
dc.date.issued 2020
dc.date.submitted 2020-05-28
dc.identifier Univerzitní knihovna (studovna) cze
dc.identifier.uri https://hdl.handle.net/10195/75965
dc.description.abstract Byla provedena rozsahla literarni re.er.e zam..ena na metody syntezy a popsane biologicke aktivity salicylamid., na mo.nosti syntezy peptid. v.etn. pou.itych .inidel, aditiv a aspekt. racemizace substratu, a na molekuly schopne inhibice proteasomu. Bylo navr.eno a experimentaln. ov..eno n.kolik mo.nych p.istup. ke konstrukci salicylamid. s peptidovym .et.zcem, ktere navazuji a roz.i.uji sou.asne znalosti v teto oblasti. Byla vybrana nejvhodn.j.i synteticka metoda, ktera byla dale optimalizovana zejmena za u.elem omezeni racemizace. Byla provedena synteza serie slou.enin odvozenych od substituovane kyseliny salicylove a dipeptid., ktere byly vhodnym zp.sobem charakterizovany (1H a 13C NMR, I., HRMS v uspo.adani MALDI-TOF, CHN analyza). Dale bylo provedeno testovani jejich biologickych aktivit (antiproliferativni aktivita v..i kmen.m leukemie K562 a CEM a mnoho.etneho myelomu U266, proteasomalni inhibice U266 v.etn. selektivity v..i jednotlivym podjednotkam ?Ŕ kruhu proteasomu 20S U266 a .asovemuho pr.b.hu inhibice v r.znych koncentracich p.ipravenych salicylamid.). cze
dc.language.iso cze
dc.publisher Univerzita Pardubice cze
dc.rights Bez omezení
dc.subject alifatické salicylamidy cze
dc.subject inhibice proteasomu cze
dc.subject syntéza peptidů cze
dc.subject amidační činidla cze
dc.subject racemizace cze
dc.subject aliphatic salicylamides eng
dc.subject inhibition of proteasome eng
dc.subject peptide synthesis eng
dc.subject amidation reagents eng
dc.subject racemization eng
dc.title Návrh a syntéza nových potenciálně cytotoxicky aktivních salicylamidů cze
dc.title.alternative Design and synthesis of novel potentially cytotoxically active salicylamides eng
dc.type disertační práce cze
dc.contributor.referee Jampílek, Josef
dc.contributor.referee Krátký, Martin
dc.date.accepted 2020-06-29
dc.description.abstract-translated Extensive literary review describing biological activities and methods of salicylamide synthesis, describing peptide synthesis including used reagents, aditives and aspects of substrate racemization, and describing molecules able of proteasomal inhibition was carried out and is presented. Several synthetical strategies for salicylamide containing a peptide chain was designed and experimentaly verified. Proposed samlicylamides are extending current state of knowledge about said topic. The most suitable synthetic method was chosen and further optimized with the aim of resolve the peptide racemisation issue which occured during the synthesis. Series of salicylamides with peptide sidechain was synthesized and characterized (1H a 13C NMR, IR, HRMS in the MALDI-TOF setting, CHN analysis). Furthermore, prepared compounds were tested for their biological activities (antiproliferative activity against leukemia cell lines K562 and CEM and multiple myeloma cell line U266, proteasomal inhibition of U266 including the selectivity towards proteolytic subunits of â ring of 20S proteasome U266, time progress of proteasomal inhibition at various salicylamide concentration levels). eng
dc.description.department Fakulta chemicko-technologická cze
dc.thesis.degree-discipline Organická chemie cze
dc.thesis.degree-name Ph.D.
dc.thesis.degree-grantor Univerzita Pardubice. Fakulta chemicko-technologická cze
dc.identifier.signature D40327
dc.thesis.degree-program Organická chemie cze
dc.identifier.stag 40634
dc.description.grade Dokončená práce s úspěšnou obhajobou cze


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