Naslov
Synthesis and comparative cytostatic activity of the new N-7 acyclic purine nucleoside analogues with natural N-9 regioisomers

Autori
Prekupec, Svjetlana ; Kalokira, Blanka ; Grdiša, Mira ; Pavelić, Krešimir ; De Clercq, Erik ; Mintas, Mladen ; Raić-Malić, Silvana

Izvornik
Heterocycles (0385-5414) 65 (2005), 4; 787-796

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
Acyclic Purine Nucleoside Analogues ; Biological Evaluation ; 1H and 13C NMR Spectra

Sažetak
The synthesis of the purine derivatives alkylated at N-7 (2a) and N-9 (2b) with 2-acetoxyethoxymethyl side chain, and chemical transformations of keto to chloro (5a), chloro to thio (6a) at C-6, and amino to fluoro (7a) at C-2 position of the purine ring were described. Structures of compounds were elucidated by analysis of their 1H and 13C NMR spectra, MS spectra and elemental analyses. N-7 Regioisomers (2a-7a) were evaluated for their cytostatic activities and their inhibitory effects were compared with those of the corresponding N-9 isomers. The 2-aminopurin-6-thione derivative (6a) showed the highest cytostatic activity, particularly against murine leukemia (L1210).

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA