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Sinteza i biomedicinska ispitivanja novih bioizostera stiril-laktona i antitumorskog agensa tiazofurina

Synthesis and biomedicinal investigation of novel styryl lactone and antitumor agent tiazofurin bioisosteres

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2018
Disertacija.pdf (5.852Mb)
IzvestajKomisije.pdf (406.3Kb)
Author
Svirčev, Miloš
Mentor
Popsavin, Mirjana
Committee members
Popsavin, Velimir
Popsavin, Mirjana
Kojić, Vesna
Popović, Boris
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Abstract
U ovom radu prikazana je sinteza 11 tiazolnih izostera goniofufurona (1-11), 4 konformaciono kruta analoga goniofufurona (12-15) i jednog butadiolnog derivata  tiazofurina  (16).  Takođe,  izvršeno  je  ispitivanje  i  poređenje bioloških  aktivnosti  sintetisanih  analoga  sa  sa  aktivnošću  i  selektivnošću kako GF i TF tako i doksorubicina, jedinjenja širokog spektra dejstva (DOX). Hiralni  prekursor  novosintetisanih  jedinjenja  1-15  bila  je  D-glukoza,  a jedinjenja 16 D-arabinoza.
A multistep synthesis of 11 novel thiazole isosteres of goniofufurone (1-11), 4 novel conformationally constrained isosteres of goniofufurone (12-15), as well as  one  butanediole  derivative  of  tiazofurin  (16)  has  been  achieved.  In  vitro cytotoxicity of newly synthetized derivatives has been evaluated and compared with the cytotoxicities of goniofufurone, tiazofurin and doxorubicin.
Faculty:
University of Novi Sad, Faculty of Science
Date:
26-09-2018
Projects:
  • Synthesis and biological testing of new mimics or derivatives of selected cytotoxic lactones, antitumor agent tiazofurin and natural naphthenic acids (RS-172006)
  • Bioactive natural products as potential sources of new pharmaceuticals and food supplements (RS-172058)
Keywords:
(+)-Goniofufuron / (+)-Goniofufurone / tiazofurin / cytotoxic lactones / C-nucleosides / D-glucose / Darabinose / tiazofurin / citotoksični laktoni / C-nukleozidi / D-glukoza / Darabinoza.
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https://www.cris.uns.ac.rs/DownloadFileServlet/Disertacija153190153401444.pdf?controlNumber=(BISIS)107610&fileName=153190153401444.pdf&id=11729&source=NaRDuS&language=sr
http://nardus.mpn.gov.rs/handle/123456789/10366
https://www.cris.uns.ac.rs/record.jsf?recordId=107610&source=NaRDuS&language=sr
https://www.cris.uns.ac.rs/DownloadFileServlet/IzvestajKomisije15319015464675.pdf?controlNumber=(BISIS)107610&fileName=15319015464675.pdf&id=11730&source=NaRDuS&language=sr

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