450356-77-1Relevant articles and documents
Parallel synthesis of pteridine derivatives as potent inhibitors for hepatitis C virus NS5B RNA-dependent RNA polymerase
Ding, Yili,Girardet, Jean-Luc,Smith, Kenneth L.,Larson, Gary,Prigaro, Brett,Lai, Vicky C.H.,Zhong, Weidong,Wu, Jim Z.
, p. 675 - 678 (2005)
From compound library screening using an HCV NS5B RNA-dependent RNA polymerase enzymatic assay, we identified a pteridine hit compound with an IC50 of 15 μM. Our SAR studies were focused on the different groups at the 6- and 7-positions, substitutions at the 4-position, and replacement of N1 or N3 with carbon in the pteridine ring. We found that NH or OH at 4-position is critical for the inhibitory activity. Furthermore, a hydrophobic substituent at the 4-position may help compounds permeate through the cell membrane.