Designed Spiro-Bicyclic Analogues Targeting the Ribosomal Decoding Center (pages 71–87)
Dr. Thomas Cottin, Dr. Constantina Pyrkotis, Dr. Christos I. Stathakis, Ioannis Mavridis, Dr. Ioannis A. Katsoulis, Panoula Anastasopoulou, Dr. Georgia Kythreoti, Dr. Alexandros L. Zografos, Dr. Victoria R. Nahmias, Dr. Athanasios Papakyriakou and Dr. Dionisios Vourloumis
Version of Record online: 8 DEC 2010 | DOI: 10.1002/cbic.201000591
Mimicking aminoglycosides: An optimized approach has been developed for the synthesis of rigid 5,6-, 6,6- and 7,6-bicyclic scaffolds that mimic many of the interactions of the natural aminoglycosides for the ribosomal decoding center. Their binding affinities for the A-site along with their potential to inhibit protein production in vitro are presented. Our results comprise useful SAR observations for structure-based drug design specific for RNA constructs.