Sinteza i karakterizacija novih urea klorokina s aminoalkoholima

master's thesis

• Title (english): Synthesis and charachterisation of new urea derivatives of chloroquine and aminoalcohols
• Author: Branimir Plavša
• Mentor: Zrinka Rajić (mentor)
• Committee member: Zrinka Rajić (predsjednik povjerenstva)
• Committee member: Branka Zorc (član povjerenstva)
• Committee member: Davor Šakić (član povjerenstva)
• Granter: University of Zagreb; Faculty of Pharmacy and Biochemistry; (Department of medicinal chemistry); Zagreb
• Defense date and country: 2019-05-17, Croatia
• Scientific / art field, discipline and subdiscipline: BIOMEDICINE AND HEALTHCARE; Pharmacy; Pharmacy

Abstract

Klorokin je antimalarijski lijek za kojeg je poznato da ima i antitumorsko djelovanje. U ovom radu dan je pregled
literaturnih podataka o antitumorskom djelovanju antimalarika, s naglaskom na klorokinu, kao i o njihovom
potencijalu da posluže kao spojevi uzori za sintezu novih antitumorskih lijekova. Detaljnije je opisan proces
autofagije, budući da se smatra da je glavni mehanizam kojim klorokin inhibira preživljavanje stanica raka vezan uz
inhibiciju autofagije. U svrhu daljnjeg istraživanja potencijalne antitumorske aktivnosti derivata klorokina sintetizirano
je 5 novih spojeva: BtcCQ (3) i uree 4a-d. Novosintetizirani spojevi su okarakterizirani uobičajenim analitičkim
tehnikama (IR, MS, 1H i 13C NMR). Spojevi 3 i 4a-d u potpunosti odgovaraju Lipinskijevim, Gelovanijevim i
Veberovim pravilima, odnosno kriterijima alata Bioavailability radar (SwissAdme). U daljnjim istraživanjima, koja
prelaze okvire ovoga diplomskog rada, bit će ispitano njihovo citostatsko djelovanje.

Abstract (english)

Chloroquine is an antimalarial drug with well-known cytostatic properties. This thesis gives an overview of the current
literature regarding the cytotoxic activity of antimalarials and their potential to serve as lead compounds for the
synthesis of new anticancer agents. The process of autophagy is described in more detail since it is believed that
chloroquine owes its anticancer activity to the inhibition of autophagy. Five novel chloroquine derivatives were
synthesized: BtcCQ (3) and ureas 4a-d. Newly synthesized compounds were characterized by standard analytical
techniques (IR, MS, 1H and 13C NMR). Compounds 3 and 4a-d comply with Lipinski, Gelovani and Veber rules, as
well as with the criteria of Bioavailability radar (SwissAdme). Future investigations will focus on the evaluation of
their cytostatic activity.

• Keywords: klorokin; urea; sinteza
• Keywords (english): chloroquine; urea; synthesis
• Language: croatian
• URN:NBN: urn:nbn:hr:163:807097
• Study programme: Title: Pharmacy; Study programme type: university; Study level: integrated undergraduate and graduate; Academic / professional title: magistar/magistra farmacije (magistar/magistra farmacije)
• Type of resource: Text
• File origin: Born digital
• Access conditions: Open access
• Created on: 2020-02-12 13:15:51