Document Detail

Design and synthesis of novel nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors from caffeic acid phenethyl ester.
MedLine Citation:
PMID:  19625188     Owner:  NLM     Status:  MEDLINE    
A series of nitrogen-containing polyhydroxylated aromatics from caffeic acid phenethyl ester were designed and synthesized as HIV-1 integrase inhibitors. Most of these compounds exhibited potent inhibitory activities at micromolar concentrations against HIV-1 integrase in the 3'-end processing and the strand transfer. Their key structure-activity relationship was also discussed.
Peng Wang; Chuan Liu; Tino Sanches; Yuan Zhong; Bo Liu; Junlong Xiong; Nouri Neamati; Guisen Zhao
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-07-03
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  19     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2009 Aug 
Date Detail:
Created Date:  2009-07-29     Completed Date:  2009-10-13     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  4574-8     Citation Subset:  IM    
School of Pharmaceutical Sciences, Shandong University, Ji'nan, Shandong Province 250012, PR China.
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MeSH Terms
Caffeic Acids / chemistry*
Drug Design
HIV Integrase / chemistry*,  metabolism
HIV Integrase Inhibitors / chemical synthesis*,  chemistry,  pharmacology
Nitrogen / chemistry
Phenylethyl Alcohol / analogs & derivatives*,  chemistry
Structure-Activity Relationship
Reg. No./Substance:
0/Caffeic Acids; 0/HIV Integrase Inhibitors; 0/p31 integrase protein, Human immunodeficiency virus 1; 104594-70-9/caffeic acid phenethyl ester; 60-12-8/Phenylethyl Alcohol; 7727-37-9/Nitrogen; EC 2.7.7.-/HIV Integrase

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