Novel 1, 2, 4-triazole and purine acyclic cyclopropane nucleoside analogues : synthesis, antiviral and cytostatic activity evaluations (CROSBI ID 170416)
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Podaci o odgovornosti
Benci, Krešimir ; Suhina, Tomislav ; Mandić, Leo ; Kraljević Pavelić, Sandra ; Tomljenović Paravić, Andrea ; Pavelić, Krešimir ; Balzarini, Jan ; Wittine, Karlo ; Mintas, Mladen
engleski
Novel 1, 2, 4-triazole and purine acyclic cyclopropane nucleoside analogues : synthesis, antiviral and cytostatic activity evaluations
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).
acyclic nucleoside analogues; synthesis; antiviral evaluation; cytostatic evaluation
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Podaci o izdanju
Povezanost rada
Kemija, Temeljne medicinske znanosti