Naslov
Novel 1, 2, 4-triazole and purine acyclic cyclopropane nucleoside analogues : synthesis, antiviral and cytostatic activity evaluations

Autori
Benci, Krešimir ; Suhina, Tomislav ; Mandić, Leo ; Kraljević Pavelić, Sandra ; Tomljenović Paravić, Andrea ; Pavelić, Krešimir ; Balzarini, Jan ; Wittine, Karlo ; Mintas, Mladen

Izvornik
Antiviral Chemistry & Chemotherapy (0956-3202) 21 (2011), 6; 221-230

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

Ključne riječi
acyclic nucleoside analogues; synthesis; antiviral evaluation; cytostatic evaluation

Sažetak
Herein we report the synthesis of novel types of 1, 2, 4-triazole (9-11 and 13) and purine (12, and 14–17) acyclic cyclopropane nucleoside analogues, containing a flexible methylenic spacer between the heterocyclic base and the carbocyclic moiety and their antiviral and cytostatic activity evaluation against malignant tumor cell lines and normal human fibroblasts (WI38). None of the compounds showed pronounced antiviral activity at subtoxic concentrations. The lack of antiherpetic activity may be due to a poor if any recognition of the compounds by the virus-induced nucleoside kinases to become metabolically activated. The in vitro cytostatic activity evaluation results indicated a weak antiproliferative activity for all tested compounds. Only 6-pyrrolylpurine derivative bearing a carboxy group substituted cyclopropane ring (17) produced a rather slight inhibitory effect at higher micromolar concentrations on breast carcinoma cell line (MCF-7) and no cytotoxic effect on human normal fibroblasts (WI 38).

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti

POVEZANOST RADA