Biological evaluation of hepatitis C virus helicase inhibitors.
A small chemical library has been synthesized and assayed for inhibition of HCV helicase activity. This study provides the structure-activity relationship of the reported inhibitors, with emphasis placed on the aminophenylbenzimidazole moiety and the linkers. Our data highlight the importance of preserving the aminophenylbenzimidazole core and the hydrophobic linkers for biological activity. The development of a robust HCV helicase assay is also described.
Phoon
C W
CW
Medicinal and Combinatorial Chemistry Laboratory, Institute of Molecular and Cell Biology, 30Medical Drive, 117609, Singapore.
Ng
P Y
PY
Ting
A E
AE
Yeo
S L
SL
Sim
M M
MM
D001562:Benzimidazoles / Q000737:chemistry; D004265:DNA Helicases / Q000037:antagonists & inhibitors*; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D016174:Hepacivirus / Q000201:enzymology*; D009682:Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization
D001562:Benzimidazoles; D004791:Enzyme Inhibitors; D004265:DNA Helicases