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Pregled bibliografske jedinice broj: 761803

Zbornik radova

Autori: Gregorić, Tomislav; Bistrović, Andrea; Tomljenović Paravić, Andrea; Sedić, Mirela; Kraljević Pavelić, Sandra; Gazivoda Kraljević, Tatjana; Raić-Malić, Silvana
Naslov: Derivati purinskih bioizostera i pirimidina s 1, 2, 3- triazolom kao farmakoforom
( 1, 2, 3-triazole pharmacophore-based derivatives of purine bioisosteres and pyrimidines )
Izvornik: / Ukić, Šime ; Bolanča, Tomislav (ur.). - Zagreb : HDKI/CSCE , 2015. 185-185 (ISBN: 978-953-6894-54-3).
Skup: XXIV. hrvatski skup kemičara i kemijskih inženjera
Mjesto i datum: Zagreb, Hrvatska, 21.-24.04.2015.
Ključne riječi: 1 ; 2 ; 3-triazoli ; purinski bioizosteri ; cikloadicija alkina i azida ; citostatska djelovanja
( 1 ; 2 ; 3-triazoles ; purine bioisosteres ; alkyne-azide cycloaddition ; cytostatic activity )
Sažetak:
Introduction of a 1, 2, 3-triazole ring into nucleosides to improve their bioactivity for antitumor or antiviral applications has become wide spread. The click chemistry reactions of nucleosides and nucleotides have found wide application in lead identification and lead optimization procedures in drug design. The 1, 2, 3- triazole unit may be considered as a surrogate of the amide group because it has H-bond acceptor capacity, distance between substituents and dipolar properties similar to the peptide bond. Keeping into consideration the biological potency of 1, 2, 3-triazolo-nucleosides [1, 2] and in our continuous endeavor toward the synthesis of pharmacologically active molecules, we designed the synthesized 1, 2, 3-triazole embedded N- heterocycles in order to evalute their cytostatic activities. The target regioselective 1, 4- disubstituted 1, 2, 3-triazole derivatives were prepared by the Cu-catalyzed alkyne-azide cycloaddition (CuAAC). Linear alkyl chain, substituted aromatic moiety and cyclopropyl ring were introduced as alkynyl substituents at C-5 and N-3 of pyrimidine core using palladium catalysed cross-coupling Sonogashira reaction. Evaluations of cytostatic activities of the synthesyzed compounds are currently underway.
Vrsta sudjelovanja: Poster
Vrsta prezentacije u zborniku: Sažetak
Vrsta recenzije: Domaća recenzija
Projekt / tema: HRZZ-IP-2013-11-5596
Izvorni jezik: HRV
Kategorija: Znanstveni
Znanstvena područja:
Kemija
Puni text rada: 761803.Poster_skup_kemicara.pdf (tekst priložen 15. Lip. 2015. u 13:35 sati)
Upisao u CROSBI: Silvana Raić-Malić (sraic@fkit.hr), 19. Svi. 2015. u 10:11 sati



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