sorivudine and 9-arabinofuranosylguanine

sorivudine has been researched along with 9-arabinofuranosylguanine* in 1 studies

Other Studies

1 other study(ies) available for sorivudine and 9-arabinofuranosylguanine

Article	Year
Novel selective human mitochondrial kinase inhibitors: design, synthesis and enzymatic activity. Bioorganic & medicinal chemistry, 2007, Apr-15, Volume: 15, Issue:8 Selective and effective TK2 inhibitors can be obtained by introduction of bulky lipophilic chains (acyl or alkyl entities) at the 2' position of araT and BVaraU, nucleoside analogues naturally endowed with a low TK2 affinity. These derivatives showed a competitive inhibitory activity against TK2 in micromolar range. BVaraU nucleoside analogues, modified on the 2'-O-acyl chain with a terminal N-Boc amino-group, conserved or increased the inhibitory activity against TK2 (7l and 7m IC(50): 6.4 and 3.8 microM, respectively). The substitution of an ester for a carboxamide moiety at the 2' position of araT afforded a consistent reduction of the inhibitory activity (25, IC(50): 480 microM). On the contrary, modifications at 2'-OH position of araC and araG, have provided inactive derivatives against TK2 and dGK, respectively. The biological activity of a representative compound, 2'-O-decanoyl-BVaraU, was also investigated in normal human fibroblasts and was found to impair mitochondrial function due to TK2 inhibition. Topics: Antiviral Agents; Arabinonucleosides; Drug Design; Enzyme Inhibitors; Fibroblasts; Humans; Indicators and Reagents; Magnetic Resonance Spectroscopy; Mitochondria; Phosphorylation; Phosphotransferases; Phosphotransferases (Alcohol Group Acceptor); Protein-Tyrosine Kinases; Reverse Transcriptase Polymerase Chain Reaction; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; Structure-Activity Relationship; Thymidine Kinase; Viruses	2007

Article

Year

Novel selective human mitochondrial kinase inhibitors: design, synthesis and enzymatic activity.

Bioorganic & medicinal chemistry, 2007, Apr-15, Volume: 15, Issue:8

Selective and effective TK2 inhibitors can be obtained by introduction of bulky lipophilic chains (acyl or alkyl entities) at the 2' position of araT and BVaraU, nucleoside analogues naturally endowed with a low TK2 affinity. These derivatives showed a competitive inhibitory activity against TK2 in micromolar range. BVaraU nucleoside analogues, modified on the 2'-O-acyl chain with a terminal N-Boc amino-group, conserved or increased the inhibitory activity against TK2 (7l and 7m IC(50): 6.4 and 3.8 microM, respectively). The substitution of an ester for a carboxamide moiety at the 2' position of araT afforded a consistent reduction of the inhibitory activity (25, IC(50): 480 microM). On the contrary, modifications at 2'-OH position of araC and araG, have provided inactive derivatives against TK2 and dGK, respectively. The biological activity of a representative compound, 2'-O-decanoyl-BVaraU, was also investigated in normal human fibroblasts and was found to impair mitochondrial function due to TK2 inhibition.

Topics: Antiviral Agents; Arabinonucleosides; Drug Design; Enzyme Inhibitors; Fibroblasts; Humans; Indicators and Reagents; Magnetic Resonance Spectroscopy; Mitochondria; Phosphorylation; Phosphotransferases; Phosphotransferases (Alcohol Group Acceptor); Protein-Tyrosine Kinases; Reverse Transcriptase Polymerase Chain Reaction; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; Structure-Activity Relationship; Thymidine Kinase; Viruses

2007