874362-24-0Relevant academic research and scientific papers
Application of the phosphoramidate ProTide approach to the antiviral drug ribavirin
Derudas, Marco,Brancale, Andrea,Naesens, Lieve,Neyts, Johan,Balzarini, Jan,McGuigan, Christopher
experimental part, p. 2748 - 2755 (2010/06/19)
Ribavirin is a nucleoside analogue with broad antiviral activity. Here we report the synthesis and biological evaluation of novel ribavirin ProTides designed to deliver the bioactive ribavirin monophosphate into cells. Some of the compounds display activity similar to the parent nucleoside against a range of viruses. Enzymatic, cell lysate and preliminary modeling studies have been performed to investigate the lack of enhancement of potency by the ProTides, and these indicate a failure at the final, amino acid cleavage step in the ProTide activation process, leading to inefficient release of the nucleoside monophosphate.
Novel potential anticancer naphthyl phosphoramidates of BVdU: Separation of diastereoisomers and assignment of the absolute configuration of the phosphorus center
Congiatu, Costantino,Brancale, Andrea,Mason, Malcolm D.,Jiang, Wen G.,McGuigan, Christopher
, p. 452 - 455 (2007/10/03)
We have previously reported our SAR optimization of the anticancer agent thymectacin. Tuning of the parent ProTide structure initially involved the amino acid and, subsequently, the aromatic masking group on the phosphate moiety. Herein, derivatives beari
