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master's thesis
Sinteza hidroksamske kiseline hibrida primakina i cimetne kiseline
Zagreb: University of Zagreb, Faculty of Pharmacy and Biochemistry, 2018. urn:nbn:hr:163:196243
Poje, Goran
University of Zagreb
Faculty of Pharmacy and Biochemistry
Department of medicinal chemistry

Institutional repository: Repository of Faculty of Pharmacy and Biochemistry University of Zagreb

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Poje, G. (2018). Sinteza hidroksamske kiseline hibrida primakina i cimetne kiseline (Master's thesis). Zagreb: University of Zagreb, Faculty of Pharmacy and Biochemistry. Retrieved from https://urn.nsk.hr/urn:nbn:hr:163:196243

Poje, Goran. "Sinteza hidroksamske kiseline hibrida primakina i cimetne kiseline." Master's thesis, University of Zagreb, Faculty of Pharmacy and Biochemistry, 2018. https://urn.nsk.hr/urn:nbn:hr:163:196243

Poje, Goran. "Sinteza hidroksamske kiseline hibrida primakina i cimetne kiseline." Master's thesis, University of Zagreb, Faculty of Pharmacy and Biochemistry, 2018. https://urn.nsk.hr/urn:nbn:hr:163:196243

Poje, G. (2018). 'Sinteza hidroksamske kiseline hibrida primakina i cimetne kiseline', Master's thesis, University of Zagreb, Faculty of Pharmacy and Biochemistry, accessed 23 December 2024, https://urn.nsk.hr/urn:nbn:hr:163:196243

Poje G. Sinteza hidroksamske kiseline hibrida primakina i cimetne kiseline [Master's thesis]. Zagreb: University of Zagreb, Faculty of Pharmacy and Biochemistry; 2018 [cited 2024 December 23] Available at: https://urn.nsk.hr/urn:nbn:hr:163:196243

G. Poje, "Sinteza hidroksamske kiseline hibrida primakina i cimetne kiseline", Master's thesis, University of Zagreb, Faculty of Pharmacy and Biochemistry, Zagreb, 2018. Available at: https://urn.nsk.hr/urn:nbn:hr:163:196243

Metadata
TitleSinteza hidroksamske kiseline hibrida primakina i cimetne kiseline
Title (english)Synthesis of primaquine-cinammic acid hybrid with hydroxamic acid moiety
AuthorGoran Poje
MentorZrinka Rajić Džolić (mentor)
Committee memberZrinka Rajić Džolić (predsjednik povjerenstva)
Committee memberBranka Zorc (član povjerenstva)
Committee memberVišnja Drinovac (član povjerenstva)
GranterUniversity of Zagreb
Faculty of Pharmacy and Biochemistry
(Department of medicinal chemistry)
Zagreb
Defense date and country2018-06-29, Croatia
Scientific / art field,
discipline and subdiscipline		BIOMEDICINE AND HEALTHCARE
Pharmacy
Pharmacy
Abstract
Novija istraživanja pokazuju da su epigenetske modifikacije jednako bitne u procesu razvoja tumora kao i mutacije gena. Posebno se ističu acetilacije, odnosno deacetilacije jer utječu na strukturu kromatina čime određuju gensku ekspresiju. U tumorskih stanica uočena je prekomjerna aktivnost histonskih deacetilaza (HDAC) koje uklanjaju ε-acetilnu skupinu iz bočnih aminokiselinskih ogranaka lizina. Dolazi do utišavanja tumorsupresorskih gena te aktivacije gena koji potiču preživljavanje i proliferaciju stanica tumora. Lijekovi inhibitori HDAC kompleksiraju ione cinka iz aktivnog mjesta enzima. Prema kemijskoj strukturi dijelimo ih u četiri skupine, od kojih su najzanimljivije hidroksamske kiseline zbog visoke sposobnosti keliranja iona metala i inhibicije HDAC-a. Cilj ovoga diplomskog rada bila je sinteza hibridnog derivata primakina i cimetne kiseline s terminalnom hidroksamskom kiselinom, za kojeg se pretpostavlja da bi, zbog svojih strukturnih karakteristika, mogao imati antimalarijsko i/ili citostatsko djelovanje. Isprobane su tri sintetske metode, no unatoč tome, sinteza ciljne molekule nije bila uspješna.
Abstract (english)
Recent research shows that carcinogenesis cannot be explained only by genetic alterations, but also involves epigenetic modifications. In particular acetylation and deacetylation affect the structure of chromatin which determines gene expression. In tumor cells excessive activity of histone deacetylases (HDAC), enzymes that remove the ε-acetyl group from the lateral lysine amino acid residues, was observed. It results in suppression of tumor-suppressor genes and activation of genes that stimulate survival and proliferation of tumor cells. HDAC inhibitors complex zinc ions found in the enzyme's active site. According to the chemical structure, they are divided into four groups, of which hydroxamic acids are the most interesting ones, due to their high metal ion chelating ability. The goal of this diploma thesis was the synthesis of a hybrid derivative primaquine and cinnamic acid with terminal hydroxamic acid moiety, which might, due to the structural characteristics, exert cytostatic and/or antimalarial activity. Although three synthetic methods were employed, synthesis of the target compound was not achieved.
Keywords
Keywords (english)
Languagecroatian
URN:NBNurn:nbn:hr:163:196243
Study programmeTitle: Pharmacy
Study programme type: university
Study level: integrated undergraduate and graduate
Academic / professional title: magistar/magistra farmacije (magistar/magistra farmacije)
Type of resourceText
File originBorn digital
Access conditionsOpen access
Terms of useLicence In copyright icon
Created on2019-01-16 09:53:26