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Novel 1, 2, 4-triazole and purine acyclic cyclopropane nucleoside analogues: synthesis, antiviral and cytostatic activity evaluations (CROSBI ID 576697)

Prilog sa skupa u zborniku | sažetak izlaganja sa skupa | 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 // Abstracts of the International Symposium on Advances in Synthetic and Medicinal Chemistry / Nicolaou, Kyriacos Costa (ur.). Sankt Peterburg, 2011. str. 221-230

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

Several published studies indicate that the acyclic guanine nucleoside analogues possessing bis(1, 2- hydroxymethyl) substituted cyclopropane rings mimicking the sugar moiety are potent inhibitors of replication of several herpes viruses. Established synthetic methods and antiviral and cytostatic activity assays were used for the evaluation of new 1, 2, 4-triazole and purine acyclic nucleoside analogues. The synthesis of new types of acyclic nucleoside analogues which incorporate 1, 2, 4-triazole (9–11 and 13) or purine (12 and 14–17) moiety bound via flexible methylenic spacer to the bis(1, 2-hydroxymethyl) cyclopropane ring. None of the new compounds showed pronounced antiviral activities at subtoxic concentrations on a broad panel of DNA and RNA viruses. Evaluation of their affinity for herpes simplex type 1 (HSV-1) and varicella-zoster virus-encoded thymidine kinases (VZV TK) also showed that none of the compounds was able to significantly inhibit 1 μM deoxythymidine phosphorylation by HSV-1 and VZV TK at 500 μM concentrations. The in vitro cytostatic activity evaluation results indicated a weak antiproliferative activity for all tested compounds. Only 6-pyrrolylpurine derivative bearing a carboxylic group substituted cyclopropane ring (17) produced a rather slight inhibitory effect at higher micromolar concentrations on a breast carcinoma cell line (MCF-7) and no cytotoxic effect on human normal fibroblasts (WI 38). The lack of antiherpetic activity may be due to poor, if any, recognition of the compounds by the virus-induced nucleoside kinases and to become metabolically activated.

synthesis; antiviral activity evaluations; Nucleoside analogues

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Podaci o prilogu

221-230.

2011.

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objavljeno

Podaci o matičnoj publikaciji

Abstracts of the International Symposium on Advances in Synthetic and Medicinal Chemistry

Nicolaou, Kyriacos Costa

Sankt Peterburg:

Podaci o skupu

International Symposium on Advances in Synthetic and Medicinal Chemistry

poster

21.08.2011-25.08.2011

Sankt Peterburg, Ruska Federacija

Povezanost rada

Kemija