Inhibition of hepatitis C virus NS5B polymerase by S-trityl-l-cysteine derivatives
نویسندگان
چکیده
منابع مشابه
New Pyrazolobenzothiazine Derivatives as Hepatitis C Virus NS5B Polymerase Palm Site I Inhibitors
We have previously identified the pyrazolobenzothiazine scaffold as a promising chemotype against hepatitis C virus (HCV) NS5B polymerase, a validated and promising anti-HCV target. Herein we describe the design, synthesis, enzymatic, and cellular characterization of new pyrazolobenzothiazines as anti-HCV inhibitors. The binding site for a representative derivative was mapped to NS5B palm site ...
متن کاملDocetaxel-resistant prostate cancer cells remain sensitive to S-trityl-L-cysteine-mediated Eg5 inhibition.
Castrate-resistant prostate cancer remains a major clinical challenge. Due to the toxicity profile of taxane-based chemotherapy and treatment failure in some patients, novel agents with improved efficacy to side effect profiles are urgently needed. Eg5, a member of the kinesin-5 family, controls the formation of the bipolar spindle during cell division, and suppressed Eg5 function leads to mito...
متن کاملInhibition of hepatitis C virus (HCV) replication by specific RNA aptamers against HCV NS5B RNA replicase.
This study identified specific and avid RNA aptamers consisting of 2'-hydroxyl- or 2'-fluoropyrimidines against hepatitis C virus (HCV) NS5B replicase, an enzyme that is essential for HCV replication. These aptamers acted as potent decoys to competitively impede replicase-catalyzed RNA synthesis activity. Cytoplasmic expression of the 2'-hydroxyl aptamer efficiently inhibited HCV replicon repli...
متن کاملOrg . On Cysteine and Cystine Peptides . Part V . l S - Trityl - and S - Diphenyl - methyl - cysteine and - cysteine Peptides
A new method for the preparation of S-trityl(i.e. triphenylmethyl) and S-diphenylmethyl-cysteines or -cysteine peptides involves treatment of cysteine or cysteine peptides with aralkylcarbinols in the presence of trifluoroacetic acid or hydrogen halides in acetic acid solution. The optimal conditions for the removal of these S-protecting aralkyl groups by trifluoroacetic acid or hydrogen halide...
متن کاملComputational analysis of de novo evolution of hepatitis C virus NS5B polymerase inhibitors.
HCV (Hepatitis C virus) that causes chronic liver disease. HCV NS5B RNA-dependent RNA polymerase (RbRp) and NS3 protease are able to affect virtual replication of genes. Computer-aided drug design (CADD) aims at designing new molecules with pharmacological activity. In this study, we used the Discovery Studio 2.0 program and the scoring function to estimate the Dock Score, piecewise linear pote...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: European Journal of Medicinal Chemistry
سال: 2012
ISSN: 0223-5234
DOI: 10.1016/j.ejmech.2012.01.010