Document Detail

Novel N-substituted benzimidazole CXCR4 antagonists as potential anti-HIV agents.
MedLine Citation:
PMID:  20207537     Owner:  NLM     Status:  MEDLINE    
The lead optimization of a series of N-substituted benzimidazole CXCR4 antagonists is described. Side chain modifications and stereochemical optimization led to substantial improvements in potency and protein shift to afford compounds with low nanomolar anti-HIV activity.
John F Miller; Elizabeth M Turner; Kristjan S Gudmundsson; Stephen Jenkinson; Andrew Spaltenstein; Michael Thomson; Pat Wheelan
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Publication Detail:
Type:  Journal Article     Date:  2010-02-14
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  20     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2010 Apr 
Date Detail:
Created Date:  2010-03-22     Completed Date:  2010-07-05     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  2125-8     Citation Subset:  IM    
Copyright Information:
2010 Elsevier Ltd. All rights reserved.
Department of Medicinal Chemistry, Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA.
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MeSH Terms
Anti-HIV Agents / chemistry*,  pharmacology*
Benzimidazoles / chemistry*,  pharmacology*
Cell Line
HIV Infections / drug therapy*
HIV-1 / drug effects*
Inhibitory Concentration 50
Receptors, CXCR4 / antagonists & inhibitors*,  metabolism
Reg. No./Substance:
0/Anti-HIV Agents; 0/Benzimidazoles; 0/Receptors, CXCR4

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