engleski

The Novel Spacered Cyclopropyl Nucleoside Analogues : Synthesis, Structural Studies And Biological Evaluation Of The Purine Supstituted 1-Aminocyclopropane-1-Carboxylic Acids And 1- Amino-1-Hydroxymethylcyclopropanes

The novel purine derivatives of 1- aminocyclopropane-1-carboxylic acid (7, 8) and 1-amino-1-hydroxymethylcyclopropane (11, 12) containing methylene spacer between the base and the cyclopropane ring were prepared by multistep synthetic route involving alkylation of appropriately substituted purine with specifically protected methyl 1-[N-(tert- Boc)amino]-2-(O-Ts-hydroxymethyl)cyclopropane- 1-carboxylate as a key reaction. Z- configuration of the novel compounds was determined by one and two dimensional 1H and 13C NMR techniques and X-ray structure analyses. The novel compounds were evaluated on cytostatic and antiviral activities on several cell lines. The compound 11 exhibited a more pronounced inhibitory activity against the proliferation of cervical carcinoma (HeLa) and human fibroblast (WI-38) cells than other types of tumor cell lines. None of the compounds showed inhibitory activities against CMV, VZV and several other viruses.

purine derivatives

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