Linked Life Data

6887210

Source:http://linkedlifedata.com/resource/pubmed/id/6887210

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
9
pubmed:dateCreated
1983-10-8
pubmed:abstractText
2-Hydroxy-5-(3,4-dichlorophenyl)-6,7-bis(hydroxymethyl)-2,3-dihydro-1H- pyrrolizine bis(2-propylcarbamate) (11) was prepared in a multistep synthesis. The 2-hydroxy group was used to prepare ester prodrugs 14 and 15, and the antineoplastic activities of 11, 14, and 15a were compared to 1 (the 2-deoxy analogue of 11) in murine P388 lymphocytic leukemia and B16 melanocarcinoma. The alcohol 11 showed comparable activity to 1, while 14 was less active and 15a showed very low activity. The hydrolytic rates of 1, 11, 14, 15a, and 15b were compared, and it was found that the two carbamate moieties were much more susceptible toward hydrolysis than the C-2 esters. The salts 15a and 15b exhibited good water solubility, 3.0 X 10(-2) and 3.88 X 10(-2) M, respectively.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:volume
26
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1333-8
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1983
pubmed:articleTitle
Synthesis, evaluation of chemical reactivity, and murine antineoplastic activity of 2-hydroxy-5-(3,4-dichlorophenyl)-6,7-bis(hydroxymethyl)-2,3-dihydro-1H- pyrrolizine bis(2-propylcarbamate) and 2-acyloxy derivatives as potential water-soluble prodrugs.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S.