Phosphonylated Acyclic Guanosine Analogues with the 1,2,3-Triazole LinkerReportar como inadecuado




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1

Bioorganic Chemistry Laboratory, Faculty of Pharmacy, Medical University of Lodz, 90-151 Lodz, Muszyńskiego 1, Poland

2

Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium





*

Author to whom correspondence should be addressed.



Academic Editor: Maria Emília de Sousa

Abstract A novel series of {4-2-amino-6-chloro-9H-purin-9-ylmethyl-1H-1,2,3-triazol-1-yl}alkylphosphonates and {4-2-amino-6-oxo-1,6-dihydro-9H-purin-9-ylmethyl-1H-1,2,3-triazol-1-yl}alkylphosphonates as acyclic analogues of guanosine were synthesized and assessed for antiviral activity against a broad range of DNA and RNA viruses and for their cytostatic activity toward three cancerous cell lines HeLa, L1210 and CEM. They were devoid of antiviral activity; however, several phosphonates were found slightly cytostatic against HeLa cells at an IC50 in the 80–210 µM range. Compounds 1R,2S-17k and 1S,2S-17k showed the highest inhibitory effects IC50 = 15–30 µM against the proliferation of murine leukemia L1210 and human T-lymphocyte CEM cell lines. View Full-Text

Keywords: azidophosphonates; acyclonucleotides; 1,2,3-triazoles; cycloaddition; antiviral; cytostatic azidophosphonates; acyclonucleotides; 1,2,3-triazoles; cycloaddition; antiviral; cytostatic





Autor: Iwona E. Głowacka 1,* , Graciela Andrei 2, Dominique Schols 2, Robert Snoeck 2 and Dorota G. Piotrowska 1

Fuente: http://mdpi.com/



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