Synthesis and biological evaluation of L- and D-configuration 1,3-dioxolane 5-azacytosine and 6-azathymine nucleosides

  • Bioorg Med Chem Lett. 2000 Sep 18;10(18):2145-8. doi: 10.1016/s0960-894x(00)00418-2.
M Z Luo  1 ,  M C Liu ,  D E Mozdziesz ,  T S Lin ,  G E Dutschman ,  E A Gullen ,  Y C Cheng ,  A C Sartorelli
Affiliations
  • 1. Department of Pharmacology and Developmental Therapeutics Program, Cancer Center, Yale University School of Medicine, New Haven, CT 06520-8066, USA.
PMID: 10999490 DOI: 10.1016/s0960-894x(00)00418-2
Abstract

Novel L- and D-configuration dioxolane 5-azacytosine and 6-azathymine nucleosides have been synthesized and evaluated for biological activity. (-)-(2S,4S)-1-[2-(Hydroxymethyl)-1,3-dioxolan-4-yl]-5-azacytosine (6) showed significant activity against HBV, whereas the D-configuration analogue (14) has been found to exhibit potent anti-HIV activity.