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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2008-2-8
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pubmed:abstractText |
Four nucleoside analogues ( 1- 4) containing a common heterocyclic base, 4(7)-amino-6(5) H-imidazo[4,5- d]pyridazin-7(4)one, were screened against calf-intestine adenosine deaminase. Compounds 1 and 3 with K(i) values of 10-12 microM are more than four times as potent inhibitors of ADA compared with 2 and 4, with K(i) values of 51-52 microM. Also, 3 is not a substrate of ADA. Nucleosides 3 and 4 also exhibit moderate in vitro activity against breast cancer cell lines, while all four are only minimally or nontoxic to the normal cells.
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pubmed:grant |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
14
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
694-8
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:18173230-Adenosine,
pubmed-meshheading:18173230-Adenosine Deaminase Inhibitors,
pubmed-meshheading:18173230-Antineoplastic Agents,
pubmed-meshheading:18173230-Cell Line,
pubmed-meshheading:18173230-Cell Line, Tumor,
pubmed-meshheading:18173230-Cell Proliferation,
pubmed-meshheading:18173230-Drug Screening Assays, Antitumor,
pubmed-meshheading:18173230-Humans,
pubmed-meshheading:18173230-Imidazoles,
pubmed-meshheading:18173230-Inosine,
pubmed-meshheading:18173230-Pyridazines,
pubmed-meshheading:18173230-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Inhibition of adenosine deaminase by analogues of adenosine and inosine, incorporating a common heterocyclic base, 4(7)-amino-6(5)H-imidazo[4,5-d]pyridazin-7(4)one.
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pubmed:affiliation |
Laboratory for Drug Design and Synthesis, Department of Chemistry and Biochemistry, University of Maryland Baltimore County, Baltimore, MD 21250, USA.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
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