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The Novel Acyclic Nucleoside Analogues Containing a Sterically Constrained (Z)-4-amino-2-butenyl Moiety: Synthesis, Cytostatic and Antiviral Activity Evaluation


Wittine, Karlo; Benci, Krešimir; Kraljević Pavelić, Sandra; Pavelić, Krešimir; Bratulić, Siniša; Hock, Karlo; Balzarini, Jan; Mintas, Mladen
The Novel Acyclic Nucleoside Analogues Containing a Sterically Constrained (Z)-4-amino-2-butenyl Moiety: Synthesis, Cytostatic and Antiviral Activity Evaluation // XXI. Hrvatski skup kemičara i kemijskih inženjera
Trogir, Hrvatska, 2009. str. 92-92 (poster, međunarodna recenzija, sažetak, znanstveni)


Naslov
The Novel Acyclic Nucleoside Analogues Containing a Sterically Constrained (Z)-4-amino-2-butenyl Moiety: Synthesis, Cytostatic and Antiviral Activity Evaluation

Autori
Wittine, Karlo ; Benci, Krešimir ; Kraljević Pavelić, Sandra ; Pavelić, Krešimir ; Bratulić, Siniša ; Hock, Karlo ; Balzarini, Jan ; Mintas, Mladen

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
XXI. Hrvatski skup kemičara i kemijskih inženjera / - , 2009, 92-92

Skup
XXI. Hrvatski skup kemičara i kemijskih inženjera

Mjesto i datum
Trogir, Hrvatska, 19-22.04.2009

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
Acyclic nucleoside analogues; Purine and Pyrimidine derivatives; cytostatic activity; antiviral activity

Sažetak
A series of the novel pyrimidine (3-6) and purine (12-15, 18-21) acyclic nucleoside analogues in which the sugar moiety was replaced by a sterically constrained Z-4-amino-, 4-aminohydrochloride-2-butenyl, or aliphatic 4-aminohydrochloride-2-butyl moiety were synthesized and evaluated for their antiviral and cytostatic activity potency. Cytostatic evaluation of the novel compounds on selected panel of human tumour cell lines showed that the majority of compounds exerted a non-specific antiproliferative effect at the highest tested concentration (i.e. 1 x 10-4 M) against all cell lines. Nevertheless, a rather moderate but selective antiproliferative effects on HeLa cell cultures in comparison to normal fibroblasts WI 38, was observed for compounds 15 and 21. No antiviral activity was observed, except for compounds 3, 4 and 5 that showed anti-HIV activity at 50% effective concentration ranging between 29 and 96 &micro ; ; ; ; ; ; M.

Izvorni jezik
Engleski

Znanstvena područja
Kemija



POVEZANOST RADA


Projekt / tema
125-0982464-2922 - RAZVOJ NOVIH PROLIJEKOVA I LIJEKOVA PROTIV VIRUSA I RAKA (Mladen Mintas, )

Ustanove
Fakultet kemijskog inženjerstva i tehnologije, Zagreb