Document Detail

Synthesis and HIV-1 Inhibitory Activities of Dicaffeoyl and Digalloyl Esters of Quinic Acid Derivatives.
MedLine Citation:
PMID:  23210852     Owner:  NLM     Status:  Publisher    
Twenty analogues of the anti-HIV-1 integrase (IN) inhibitors dicaffeoylquinic acids (DCQAs) were prepared. Their IC(50) values for 3'-end processing and strand transfer against recombinant HIV-1IN were determined in vitro, and their cell toxicities and EC(50) against HIV-1 were measured in cells (ex vivo). Acetylated or benzylated and/or with cyclohexylidene group compounds exhibited no inhibition of integration in biochemical assays or viral replication in HIV-infected cells, with the exception of 16 and 36. Removal of these groups, however, correlated with potent inhibition. Compounds 19, 31, and 38, all digalloyls, exhibited the most robust inhibitory performance in biochemical assays as well as in cell culture and less toxicity than other molecules in the current study.
Celso O R Junior; Shawn C Verde; Carlos A M Rezende; Wiliam Caneschi; Mara R C Couri; Brenda R McDougall; W Edward Robinson; Mauro V de Almeida
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-11-26
Journal Detail:
Title:  Current medicinal chemistry     Volume:  -     ISSN:  1875-533X     ISO Abbreviation:  Curr. Med. Chem.     Publication Date:  2012 Nov 
Date Detail:
Created Date:  2012-12-5     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9440157     Medline TA:  Curr Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Juiz de Fora, MG, Brazil.
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