Document Detail


Cytotoxicity, hydrophobicity, uptake, and distribution of osmium(II) anticancer complexes in ovarian cancer cells.
MedLine Citation:
PMID:  20000847     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The cytotoxicity, hydrophobicity (log P), cellular uptake, aqueous reactivity, and extent of DNA adduct formation in the A2780 ovarian carcinoma cells for four osmium(II) arene complexes [(eta(6)-arene)Os(4-methyl-picolinate)Cl] that differ only in their arene ligands as benzene (1), p-cymene (2), biphenyl (3), or tetrahydroanthracene (4) are reported. There is a correlation between hydrophobicity (log P), cellular uptake, nucleus uptake, and cytotoxicity of the complexes, following the order 3 approximately 4 > 2 > 1, suggesting that the arene plays an important role in the biological activity of these types of compounds. Cell distribution studies using fractionation showed that all four compounds distribute similarly within cells. DNA binding of osmium did not correlate with cytotoxicity, indicating that the nature of the DNA lesion may also be crucial to activity. TEM images of ovarian cells treated with 3 revealed morphological changes associated with apoptosis with possible involvement of mitochondria.
Authors:
Sabine H van Rijt; Arindam Mukherjee; Ana M Pizarro; Peter J Sadler
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  53     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2010 Jan 
Date Detail:
Created Date:  2010-01-21     Completed Date:  2010-03-02     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  840-9     Citation Subset:  IM    
Affiliation:
Department of Chemistry, University of Warwick, Gibbet Hill Road, Coventry CV4 7AL, UK.
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MeSH Terms
Descriptor/Qualifier:
Active Transport, Cell Nucleus
Antineoplastic Agents / chemistry*,  pharmacokinetics,  pharmacology
Apoptosis / drug effects
Benzene Derivatives
Cell Death
Cell Line, Tumor
DNA / metabolism
Female
Humans
Hydrophobicity
Mitochondria / pathology
Osmium Compounds / pharmacology*,  therapeutic use
Ovarian Neoplasms / drug therapy*,  pathology
Pharmacokinetics
Grant Support
ID/Acronym/Agency:
G0701062//Medical Research Council
Chemical
Reg. No./Substance:
0/Antineoplastic Agents; 0/Benzene Derivatives; 0/Osmium Compounds; 9007-49-2/DNA

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


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