Synthesis and biological evaluation of 2′,4′- and 3′,4′-bridged nucleoside analogues

K.C. Nicolaou, S.P. Ellery, F. Rivas, K. Saye, E. Rogers, T.J. Workinger, M. Schallenberger, R. Tawatao, A. Montero, A. Hessell, F. Romesberg, D. Carson, D. Burton Bioor. Med. Chem. (2011) 19:5648-5669.
pubpic2010xxA small library of 2′,4′- and 3′,4′-bridged nucleoside analogues was synthesized and tested for antibacterial, antitumor, and antiviral activities, leading to the identification of one nucleoside that exhibited significant antiviral activity against pseudoviruses SF162 (IC50 = 7.0 μM) and HxB2 (IC50 = 2.4 μM). These findings render bridged nucleosides as credible leads for drug discovery in the anti-HIV area of research.