Linked Life Data

21375337

Source:http://linkedlifedata.com/resource/pubmed/id/21375337

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
7
pubmed:dateCreated
2011-4-7
pubmed:abstractText
About 3% of world's population is infected by the hepatitis C virus (HCV), for which prophylactic vaccine is not available yet. Nowadays, pegylated interferon-? and ribavirin are commonly used to treat HCV; unfortunately these drugs often produce significant side effects. Upon the desperate need of anti-HCV drugs, a plan to establish a new compound library was set that included leads with high antiviral activity, good hydrophilicity, yet low toxicity. Accordingly, 26 new conjugated compounds were synthesized through the chemical coupling of various 9-(?-D-ribofuranosyl)purine-8-thiones with 3-(chloromethyl)coumarins bearing various substituents. A -SCH(2)- unit was used to link the coumarin and the purine moieties. The three hydroxyl groups at the 2'-, 3'-, and 5'-positions were selectively protected with an acyl or acetal group in these coumarin-purine ribofuranosides. Their anti-HCV and cytostatic determination assays were performed, and the structure-activity relationship was established. Three conjugates in the family of 8-(coumarin-3'-yl)methylthio-9-(?-D-ribofuranos-1''-yl)purine possessed an appealing ability to inhibit HCV replication with EC(50) between 5.5 and 6.6 ?M and EC(90) of ?20 ?M. These data in the new compound library provide clues for the future in the development of anti-HCV leads for viral eradication.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
1520-4804
pubmed:author
pubmed:issnType
Electronic
pubmed:day
14
pubmed:volume
54
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2114-26
pubmed:meshHeading
pubmed:year
2011
pubmed:articleTitle
Coumarin-purine ribofuranoside conjugates as new agents against hepatitis C virus.
pubmed:affiliation
Department of Chemistry, National Tsing Hua University , Hsinchu, Taiwan 30013, ROC. jrhwu@mx.nthu.edu.tw
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't