Linked Life Data

8595123

Source:http://linkedlifedata.com/resource/pubmed/id/8595123

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
8
pubmed:dateCreated
1996-4-16
pubmed:abstractText
New alkylating anthracycline derivatives with promising antitumor activity have been synthesized. We selected two of these compounds, 4-demethoxy-N,N-bis(2 chloroethyl)-4'-methylsulfonyl-daunorubicin (FCE 27726) and 4-demethoxy-3'-deamino-3'aziridinyl-4'-methylsulfonyl daunorubicin (FCE 28729), comparing their interaction with DNA and that of the non-alkylating derivative 4-demethoxy-4'-methylsulfonyl-daunorubicin (FCE 27894). The two alkylating derivatives were more cytotoxic than idarubicin and presented low cross-resistance with doxorubicin. Both FCE 27726 and FCE 28729 were found to alkylate guanines at the N7 position in the major groove with roughly the same specificity, but at different concentrations. FCE 27726 was 10 times more potent than FCE 28729 in alkylating DNA. At higher concentrations, FCE 27726 was able to alkylate adenines, possibly at the N3 position contained in a sequence 5'-PyAA. FCE 27726, as expected, was able to form DNA interstrand cross-links either in vitro and in vivo in treated cells. FCE 28729 did not form DNA interstrand cross-links in vivo. In vitro, at high concentrations, some DNA interstrand cross-links were evident. The non-alkylating derivative FCE 27894 did not produce any alkylation or DNA interstrand cross-links either in vitro or in vivo.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
0266-9536
pubmed:author
pubmed:issnType
Print
pubmed:volume
10
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
641-53
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1995
pubmed:articleTitle
Sequence-specific DNA interactions by novel alkylating anthracycline derivatives.
pubmed:affiliation
Istituto di Ricerche Farmacologiche Mario Negri, Milan, Italy.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't