Synthesis, in vitro anti-HIV and anti-hepatitis B activities and pharmacokinetic properties of amphiphilic heterodinucleoside phosphates containing ddC and AZT

Authors
Schwendener, RA Peghini, PA Ludwig, PS Schott, H
Citation
Ra. Schwendener et al., Synthesis, in vitro anti-HIV and anti-hepatitis B activities and pharmacokinetic properties of amphiphilic heterodinucleoside phosphates containing ddC and AZT, NUCLEOS NUC, 18(4-5), 1999, pp. 949-950
Citations number
3
Categorie Soggetti
Biochemistry & Biophysics
Journal title
NUCLEOSIDES & NUCLEOTIDES
ISSN journal
07328311 → ACNP
Volume
18
Issue
4-5
Year of publication
1999
Pages
949 - 950
Database
ISI
SICI code
0732-8311(1999)18:4-5<949:SIVAAA>2.0.ZU;2-6
Abstract
Amphiphilic heterodinucleoside phosphates containing AZT and ddC as antivir al monomer were synthesized according to the hydrogenphosphonate method and evaluated in vitro against HIV. dT-N-4-pamddC was the most active (IC50 = 40 mu M, EC50 = 80 nM) and least toxic (TI = 524) dimer and it exhibited al so strong antiviral effects against eight AZT-resistant HIV strains. The dd C-containing heterodimers additionally inhibited HBV replication by 50-80 % at 50 mu M in Hep G2 2.2.15 cells.