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Pregled bibliografske jedinice broj: 324927

Zbornik radova

Autori: Gazivoda, Tatjana; Raić-Malić, Silvana; Plavec, Janez; Kraljević-Pavelić, Sandra; Pavelić, Krešimir; Balzarini, Jan; Mintas, Mladen
Naslov: Synthesis, Cytostatic and Anti-HIV Evaluations of the New Unsaturated Acyclic C-5 Pyrimidine Nucleoside Analogues
Izvornik: Magnetic Moments in Central Europe: Book of Abstracts / Makuc, Damjan ; Plavec, Janez (ur.). - Ljubljana : NMR Centre, National Institute of Chemistry , 2008. 31-31 (ISBN: 978-961-6104-10-4).
Skup: Magnetic Moments in Central Europe
Mjesto i datum: Ljubljana, Slovenija, 29-29.02.2008.
Ključne riječi: synthesis; cytostatic and anti-HIV evaluations; pyrimidine nucleoside analogues
Sažetak:
A series of the novel C-5 alkynyl pyrimidine nucleoside analogues (1-14) in wich the sugar moiety was replaced by the conformationally restricted Z- and E-2-butenyl spacer between the phthalimido and pyrimidine ring were synthesized by using Sonogashira cross-coupling reaction. Cytostatic activity evalution of the novel compounds showed that E-isomers exhibited, in general, better cytostatic activities than the corresponding Z-isomers. E-isomers 14 exhibited the best cytostatic effect against all evaluated malignant cell lines, particularly against hepatocellular carcinoma (Hep G2, IC 50 = 4.3 µ ; M). However, this compound was also cytotoxic to human normal fibroblasts (WI 38). Its Z- isomer 7 showed highly specific antiproliferative activity Hep G2 (IC 50= 18 uM) and no cytotoxicity to WI 38. Moreover, compounds 3, 4 and 14 expressed some marginal inhibitory activity against HIV-1 and HIV-2.
Vrsta sudjelovanja: Poster
Vrsta prezentacije u zborniku: Sažetak
Vrsta recenzije: Nema recenziju
Projekt / tema: 125-0982464-2922, 125-0982464-2925, 098-0982464-2393
Izvorni jezik: ENG
Kategorija: Znanstveni
Znanstvena područja:
Kemija
Upisao u CROSBI: Mladen Mintas (mmintas@fkit.hr), 11. Ožu. 2008. u 08:10 sati



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