Construction of polyamine-modified uridine and adenosine derivatives-evaluation of DNA binding capacity and cytotoxicity in vitro

Summary, in English

We here report the synthesis of the two polyamine-based nucleoside derivatives 5-{[bis-(3-aminopropyl)amino]acetamido-1-propynyl}uridine and 2-{[bis-(3-aminopropyl)amino]-acetamido-1-propynyl}adenosine. The various polyamine derivatives have been used in thermal melting analysis using DNA from herring testes, and in cellular studies using four different cell lines. The compounds were all found to be non-toxic, thus holding good promise for future use as siRNA building blocks.

• Author: Johannes Ghatnekar; Margareta Hägerlöf; Stina Oredsson; Kersti Alm; Sofi Elmroth; Tina Persson
• Department/s: Biochemistry and Structural Biology; Functional zoology; Department of Biology; Centre for Analysis and Synthesis
• Publishing year: 2007
• Language: English
• Pages: 7426-7433
• Publication/Series: Bioorganic & Medicinal Chemistry
• Volume: 15
• Issue: 23
• Links: http://dx.doi.org/10.1016/j.bmc.2007.07.030
• Document type: Journal article
• Publisher: Elsevier
• Topic: Zoology
• Keywords: Modified nucleoside; Adenosine; Uridine; Polyamine derivatives
• Status: Published
• ISBN/ISSN/Other: ISSN: 0968-0896