Linked Life Data

6946877

Source:http://linkedlifedata.com/resource/pubmed/id/6946877

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1982-2-12
pubmed:abstractText
Ten anthracyclines, including doxorubicin (DX) and daunorubicin (DNR), and eight analogs with modifications in structure or stereochemistry of the aglycone and/or the aminosugar moiety were simultaneously tested in serial vitro titration studies against human adenocarcinomas in the human tumor stem cell assay. More than a two-log range in cytotoxicity of the various anthracyclines was observed with the tumors tested. Marked individual differences in sensitivity of specific tumors (breast, lung, peritoneal) were observed for the various analogs. By assessing average effects on survival of tumor colony-forming units (TCFU) in the tumors tested, the three compounds lacking the methoxyl group in position 4 of the aglycone (4-demethoxyDX, 4-demethoxy-4'-epiDX, 4-demethoxyDNR) all proved to be more cytotoxic than their parent compounds. Compounds modified in position 4' of the aminosugar were on average either as toxic (4' epiDX) or more toxic (4'-deoxyDX and 4'-0-methylDX) to TCFU than the parent compound DX. On average, 11-deoxyDX was less toxic than DX or the other eight anthracyclines tested. The results obtained are also in good general agreement with those previously reported for anthracyclines with human tumors in xenografts or cancer patients. These antitumor results viewed in concert with toxicology studies in normal mice (including evidence of a lack of cardiac toxicity) suggest that 4'deoxyDX may prove to be a clinically useful anthracycline analog. We also conclude that use of this clinically predictive in vitro soft agar assay provides a rapid and relatively inexpensive means of simultaneously testing a large number of analogs of a parent compound against a spectrum of human tumors.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0344-5704
pubmed:author
pubmed:issnType
Print
pubmed:volume
6
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
103-9
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1981
pubmed:articleTitle
Evaluation of new anthracycline analogs with the human tumor stem cell assay.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S.