Synthesis, cytostatic activity and ADME properties of C-5 substituted and N-acyclic pyrimidine derivatives (CROSBI ID 175342)
Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija
Podaci o odgovornosti
Gazivoda Kraljević, Tatjana ; Klika, Mateja ; Kralj, Marijeta ; Martin-Kleiner, Irena ; Jurmanović, Stella ; Milić, Astrid ; Padovan, Jasna ; Raić-Malić, Silvana
engleski
Synthesis, cytostatic activity and ADME properties of C-5 substituted and N-acyclic pyrimidine derivatives
The synthesis of the novel 5-alkyl pyrimidine derivatives, 5, 6-dihydrofuro[2, 3-d]pyrimidines and 5-alkyl N-methoxymethyl pyrimidine derivatives and evaluation of their cytostatic activities are described. The mechanism of antiproliferative effect of 5-(2-chloroethyl)-substituted pyrimidine 3 that exerted the pronounced cytostatic activity was studied in further details on colon carcinoma (HCT116) cells. The cell cycle perturbation analysis demonstrated severe DNA damage (G2/M arrest) pointing to a potential DNA alkylating ability of 3. Preliminary ADME data of 3 and its 6-methylated structural congener (6-Me-3) showed their high permeability and good metabolic stability.
5-alkyl pyrimidine derivatives ; cytostatic evaluations ; cell cycle analysis ; ADME properties
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Podaci o izdanju
22 (1)
2012.
308-312
objavljeno
0960-894X
1464-3405
10.1016/j.bmcl.2011.11.009
Povezanost rada
Kemija, Temeljne medicinske znanosti