Document Detail


Linker-modified triamine-linked acridine dimers: synthesis and cytotoxicity properties in vitro and in vivo.
MedLine Citation:
PMID:  17107806     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The preparation and cytotoxicity properties of a series of N(epsilon)-substituted triamine-linked acridine dimers are described. Most acridine dimer derivatives reveal highly potent in vitro cytotoxicity properties and DNA binding activity. Several acridine dimers were selected to study their action in vivo. These acridine dimers have demonstrated a narrow safe margin, as has adriamycin, but higher maximum tolerate dose (MTD) in comparison with that of adriamycin in ICR mice. The acridine dimers also demonstrated various anit-COLO 205 solid tumor activities in vivo. Compound 1 has shown the most potent solid tumor inhibition.
Authors:
Shan-Shue Wang; Yi-Jen Lee; Shih-Chung Hsu; Hsueh-O Chang; Wei-Kung Yin; Lien-Shange Chang; Shan-Yen Chou
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2006-10-28
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  15     ISSN:  0968-0896     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2007 Jan 
Date Detail:
Created Date:  2006-12-15     Completed Date:  2007-03-13     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  735-48     Citation Subset:  IM    
Affiliation:
Department of Biochemical Engineering, Kao Yuan University, 1821 Chung-Shan Rd, Lu-Chu Hsiang, Kaohsiung, Taiwan, ROC. sswang@cc.kyu.edu.tw
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MeSH Terms
Descriptor/Qualifier:
Acridines / chemical synthesis*,  pharmacology*
Animals
Antineoplastic Agents / chemical synthesis*,  pharmacology*
Cell Line, Tumor
Cell Survival / drug effects
Colonic Neoplasms / drug therapy,  pathology
DNA / metabolism
Humans
Indicators and Reagents
Intercalating Agents / chemical synthesis,  pharmacology
Magnetic Resonance Spectroscopy
Mass Spectrometry
Mice
Mice, Inbred ICR
Mice, SCID
Nitrogen / chemistry
Plasmids / drug effects,  genetics
Structure-Activity Relationship
Tetrazolium Salts
Thiazoles
Chemical
Reg. No./Substance:
0/Acridines; 0/Antineoplastic Agents; 0/Indicators and Reagents; 0/Intercalating Agents; 0/Tetrazolium Salts; 0/Thiazoles; 298-93-1/thiazolyl blue; 7727-37-9/Nitrogen; 9007-49-2/DNA

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


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