Synthesis and Biological Evaluation of 2-(2-Deoxy-D-erythro-pent-1-enofuranosyl)pyridine C-Nucleosides |
| |
| Authors: | E. De Vos E. L. Esmans J. A. Lepoivre F. C. Alderweireldt R. A. Dommisse P. François |
| |
| Affiliation: | 1. University of Antwerp (RUCA), Laboratory for Organic Chemistry , Groenenborgerlaan 171, B-2020, Antwerp, BELGIUM;2. Université de Louvain, Département de Chimie , Place Louis Pasteur, 1, B-1348, Louvain-La-Neuve, BELGIUM |
| |
| Abstract: | Abstract 2-(2-Deoxy-D-erythro-pent-1-enofuranosyl)pyridine and its methyl analogues have been prepared by treatment of the corresponding 2′,3′-O-isopropylidene-D-ribofuranosyl derivatives with several bases such as sodium amide, tert.BuOK, EtONa, lithium tetramethylpiperidide (LTMP) and phenyl lithium (PhLi). PhLi and tert.BuOK gave the best results. The products thus obtained showed cytostatic activity against human tumor cell lines, in particular MT-4, a human T-lymphocyte cell line. No antiviral activity was noted at subtoxic concentrations. |
| |
| Keywords: | |
|
|
