Linked Life Data

12139456

Source:http://linkedlifedata.com/resource/pubmed/id/12139456

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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
16
pubmed:dateCreated
2002-7-25
pubmed:abstractText
Novel 1,4,7-triazacyclononane-N,N',N' '-triacetic acid (NOTA) based octadentate ligands [2-(4,7-biscarboxymethyl[1,4,7]triazacyclononan-1-ylethyl)carbonylmethylamino]acetic acid tetrahydrochloride (1) and [3-(4,7-biscarboxymethyl[1,4,7]triazacyclononan-1-yl-propyl)carbonylmethylamino]acetic acid tetrahydrochloride (2) with pendent donor groups as potential yttrium chelators for radioimmunotherapy (RIT) have been prepared via a convenient and high-yield cyclization route. The complexation kinetics of the novel chelates with Y(III) was investigated and compared to that of 1,4,7,10-tetraazacyclododecane-N,N',N' ',N" '-tetraacetic acid (DOTA), a macrocyclic chelating agent well recognized as forming very stable complexes with yttrium but also limited in usage because of slow Y(III) complex formation rates. The in vitro stability of the corresponding (88)Y-labeled complexes in human serum was assessed by measuring the release of (88)Y from the complexes over 14 days. The in vivo biodistribution of (86)Y-labeled 1 in mice was evaluated and compared to that of the (86)Y-DOTA complex. Formation of the Y complex of 1 was significantly more rapid than that of either 2 or DOTA. Serum stability of the (88)Y complex formed with 1 was equivalent to the DOTA complex, while the complex formed with 2 proved to be significantly unstable. The results obtained from a biodistribution study indicate that the (86)Y-1 complex possesses in vivo stability comparable to the analogous DOTA complex.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:day
1
pubmed:volume
45
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
3458-64
pubmed:dateRevised
2004-11-17
pubmed:meshHeading
pubmed:year
2002
pubmed:articleTitle
Synthesis and biological evaluation of novel macrocyclic ligands with pendent donor groups as potential yttrium chelators for radioimmunotherapy with improved complex formation kinetics.
pubmed:affiliation
Chemistry Section, Radiation Oncology Branch, Building 10, Room B3B69, National Cancer Institute/NIH, Bethesda, MD 20892, USA.
pubmed:publicationType
Journal Article