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

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

Affiliation

  • 1 Department of Pharmacology and Developmental Therapeutics Program, Cancer Center, Yale University School of Medicine, New Haven, CT 06520-8066, USA.
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.

Figures