Document Detail


Anti-AIDS agents. Part 56: Synthesis and anti-HIV activity of 7-thia-di-O-(-)-camphanoyl-(+)-cis-khellactone (7-thia-DCK) analogs.
MedLine Citation:
PMID:  15556756     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Two thia-DCK analogs (3a,b) were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. Compound 3a showed potent anti-HIV activity with an EC50 value of 0.14 microM and a therapeutic index of 1110. However, the corresponding 6-tert-butyl-substituted compound (3b) showed no suppression. The bioassay results indicated that thia-DCK analogs merit attention as potential HIV-1 inhibitors.
Authors:
Ying Chen; Qian Zhang; Beina Zhang; Peng Xia; Yi Xia; Zheng-Yu Yang; Nicole Kilgore; Carl Wild; Susan L Morris-Natschke; Kuo-Hsiung Lee
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  12     ISSN:  0968-0896     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2004 Dec 
Date Detail:
Created Date:  2004-11-23     Completed Date:  2005-05-19     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  6383-7     Citation Subset:  IM    
Affiliation:
Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 200032, China.
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MeSH Terms
Descriptor/Qualifier:
Anti-HIV Agents / chemical synthesis*,  pharmacology
Cell Line
HIV / drug effects
Humans
Inhibitory Concentration 50
Lactones / chemical synthesis,  pharmacology
Lymphocytes / virology
Structure-Activity Relationship
Thiones / chemical synthesis,  pharmacology
Grant Support
ID/Acronym/Agency:
AI-33066/AI/NIAID NIH HHS
Chemical
Reg. No./Substance:
0/Anti-HIV Agents; 0/Lactones; 0/Thiones

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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