The Synthesis and Biological Evaluation of Sulfamoyl Nucleosides Related to Carbovir and AZT

Abstract
A series of 5′-0-sulfamoylated carbocyclic 2′,3′-dideoxy nucleosides was synthesized and evaluated for antitumor and anti-HIV activities. In this study, we have combined the phosphate mimicking features of the sulfamoyl group with our previously reported antiviral carbocyclic nucleoside, carbovir. In a related strategy, the sufamoyl moiety was used as a replacement for the α-phosphate of AZT-triphosphate in an analog designed to examine a membrane permeable HIV reverse transcriptase inhibitor. Some of the analogs exhibited significant in vitro anticancer activity.