Document Detail


Synthesis, characterization, and reaction pathways for the formation of a GMP adduct of a cytotoxic thiocyanato ruthenium arene complex.
MedLine Citation:
PMID:  19499253     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The organoruthenium complex [(eta(6)-hmb)Ru(en)(Cl)][PF6] (hmb is hexamethylbenzene, en is ethylenediamine) undergoes facile aquation and then reacts with KSCN in unbuffered solution to give the S-coordinated thiocyanato product [(eta(6)-hmb)Ru(en)(S-SCN)]+ which slowly converts to the thermodynamically favored N-bound complex [(eta(6)-hmb)Ru(en)(N-NCS)]+ (1+). Complex 1 was synthesized and characterized by X-ray crystallography and mass spectrometry. Despite its lack of hydrolysis over 24 h, complex 1 exhibits moderate cytotoxicity (IC(50) 24 microM) towards the human ovarian cancer cell line A2780, comparable with that of the chlorido analogue which is thought to be activated (towards potential target DNA) via a rapid aquation (Wang et. al. in Proc Natl Acad Sci USA 102:18269-18274, 2005). Detailed kinetic studies suggest that complex 1 binds to guanosine 5'-monophosphate (GMP) through direct N7 substitution of the N-bound SCN ligand. In the presence of a high concentration of chloride (104 mM), however, complex 1 may bind partly to GMP via Cl substitution.
Authors:
Fuyi Wang; Abraha Habtemariam; Erwin P L van der Geer; Robert J Deeth; Robert Gould; Simon Parsons; Peter J Sadler
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-06-05
Journal Detail:
Title:  Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry     Volume:  14     ISSN:  1432-1327     ISO Abbreviation:  J. Biol. Inorg. Chem.     Publication Date:  2009 Sep 
Date Detail:
Created Date:  2009-09-17     Completed Date:  2009-12-29     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9616326     Medline TA:  J Biol Inorg Chem     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  1065-76     Citation Subset:  IM    
Affiliation:
Beijing National Laboratory for Molecular Sciences, Institute of Chemistry, Chinese Academy of Sciences, 100190 Beijing, China. fuyi.wang@iccas.ac.cn
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MeSH Terms
Descriptor/Qualifier:
5'-Guanylic Acid / chemistry*
Antineoplastic Agents / chemical synthesis*,  chemistry,  pharmacology
Cell Line, Tumor
Chromatography, High Pressure Liquid
Computational Biology
Crystallography, X-Ray
Humans
Hydrolysis
Inhibitory Concentration 50
Kinetics
Models, Molecular
Molecular Structure
Organometallic Compounds / chemical synthesis,  chemistry*,  pharmacology
Ruthenium / chemistry*
Spectrometry, Mass, Electrospray Ionization
Spectrophotometry
Thiocyanates / chemical synthesis,  chemistry*,  pharmacology
Time Factors
Chemical
Reg. No./Substance:
0/Antineoplastic Agents; 0/Organometallic Compounds; 0/Thiocyanates; 7440-18-8/Ruthenium; 85-32-5/5'-Guanylic Acid

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