Document Detail


Tri- and tetra-substituted naphthalene diimides as potent G-quadruplex ligands.
MedLine Citation:
PMID:  18243701     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A series of tri- and tetra-substituted naphthalene diimides have been designed and synthesized. Several compounds show exceptional affinity for telomeric G-quadruplex DNA in classical and competition FRET assays and SPR studies. They inhibit telomerase in the TRAP assay, and show potent senescence-based short-term anti-proliferative effects on MCF7 and A549 cancer cell lines, and localize in the nucleus and particularly the nucleolus of MCF7 cells.
Authors:
Francisco Cuenca; Olga Greciano; Mekala Gunaratnam; Shozeb Haider; Deeksha Munnur; Rupesh Nanjunda; W David Wilson; Stephen Neidle
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2008-01-18
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  18     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2008 Mar 
Date Detail:
Created Date:  2008-03-10     Completed Date:  2008-05-19     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  1668-73     Citation Subset:  IM    
Affiliation:
CRUK Biomolecular Structure Group, The School of Pharmacy, University of London, 29/39 Brunswick Square, London WC1N 1AX, UK.
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MeSH Terms
Descriptor/Qualifier:
Antineoplastic Agents / chemistry*,  metabolism*,  pharmacology
Cell Line, Tumor
Fluorescence Resonance Energy Transfer
G-Quadruplexes*
Humans
Imides
Ligands
Models, Molecular
Molecular Structure
Naphthalenes
Phenanthrolines / chemistry*,  metabolism*,  pharmacology
Telomerase / antagonists & inhibitors
Chemical
Reg. No./Substance:
0/Antineoplastic Agents; 0/Imides; 0/Ligands; 0/Naphthalenes; 0/Phenanthrolines; 22291-04-9/naphthalenediimide; EC 2.7.7.49/Telomerase

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