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Novel 1, 2, 4-triazole and purine acyclic cyclopropane nucleoside analogues : synthesis, antiviral and cytostatic activity evaluations (CROSBI ID 170416)

Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija

Benci, Krešimir ; Suhina, Tomislav ; Mandić, Leo ; Kraljević Pavelić, Sandra ; Tomljenović Paravić, Andrea ; Pavelić, Krešimir ; Balzarini, Jan ; Wittine, Karlo ; Mintas, Mladen Novel 1, 2, 4-triazole and purine acyclic cyclopropane nucleoside analogues : synthesis, antiviral and cytostatic activity evaluations // Antiviral chemistry & chemotherapy, 21 (2011), 6; 221-230. doi: 10.3851/IMP1762

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

21 (6)

2011.

221-230

objavljeno

0956-3202

10.3851/IMP1762

Povezanost rada

Kemija, Temeljne medicinske znanosti

Poveznice
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