Antiviral and cytostatic evaluation of the novel 6-acyclic chain substituted thymine derivatives (CROSBI ID 116690)
Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija
Podaci o odgovornosti
Prekupec, Svjetlana ; Makuc, Damjan ; Plavec, Janez ; Kraljević, Sandra ; Kralj, Marijeta ; Pavelić, Krešimir ; Andrei, Graciela ; Snoeck, Robert ; Balzarini, Jan ; De Clercq, Erik ; Raić-Malić, Silvana ; Mintas, Mladen
engleski
Antiviral and cytostatic evaluation of the novel 6-acyclic chain substituted thymine derivatives
A series of the novel 5-methyl pyrimidine derivatives with an acyclic side chain at the C-6 position were synthesized using lithiation of a 2, 4-dimethoxy-5, 6-dimethyl pyrimidine and subsequent nucleophilic addition or substitution reactions of the organolithium intermediate thus obtained with acetaldehyde, epichlorhydrine, fluorinated ketones and fluorinated ester. The novel compounds were evaluated on their cytostatic and antiviral activities. Among all the compounds evaluated, two fluorinated acyclic pyrimidine derivatives showed the highest cytostatic activities. The compound containing a 2-hydroxy-3, 3, 3-trifluoro-1-propenyl side chain exhibited a pronounced effect against breast carcinoma (MCF-7, IC50 = 8.38 ug/ml), while the compound with 1 2-fluoromethyl-2-acetoxypropyl chain exhibited moderate effect against cervical carcinoma (HeLa, IC50 = 19.73 ug/ml).
C-6 fluoroalkylated pyrimidine derivatives ; conformational analysis ; antiviral activity ; cytostatic activity ; apoptosis
nije evidentirano
nije evidentirano
nije evidentirano
nije evidentirano
nije evidentirano
nije evidentirano
Podaci o izdanju
16 (5)
2005.
327-338
objavljeno
0956-3202
10.1177/095632020501600505
Povezanost rada
Biologija, Kemija, Temeljne medicinske znanosti