Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
13
|
pubmed:dateCreated |
1999-1-29
|
pubmed:abstractText |
The presence of an alkyl substituent at N3 in the oxazaphosphorine ring stabilizes N-substituted 4-(alkylthio)cyclophosphamides from spontaneous decomposition. Based on this finding, N3-methyl-mafosfamide was synthesized and examined as a chemically stable, biooxidative prodrug of mafosfamide. This prodrug was stable in aqueous buffer (pH 7.4, 37 degrees C) and underwent N-demethylation in a time dependent manner when incubated with rat hepatic microsomes. N3-Methyl-mafosfamide was 10-fold more cytotoxic in vitro than cyclophosphamide against mouse embryo Balb/c 3T3 cells (LC50 = 3.6 microM). Preliminary in vivo antitumor evaluation against L1210 leukemia in mice showed that this prodrug was active [Increase of life span (ILS) > 29%].
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Jul
|
pubmed:issn |
0960-894X
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
7
|
pubmed:volume |
8
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1673-8
|
pubmed:dateRevised |
2003-11-14
|
pubmed:meshHeading |
pubmed-meshheading:9873412-3T3 Cells,
pubmed-meshheading:9873412-Animals,
pubmed-meshheading:9873412-Antineoplastic Agents,
pubmed-meshheading:9873412-Cyclophosphamide,
pubmed-meshheading:9873412-Leukemia L1210,
pubmed-meshheading:9873412-Mice,
pubmed-meshheading:9873412-Mice, Inbred BALB C,
pubmed-meshheading:9873412-Prodrugs,
pubmed-meshheading:9873412-Rats,
pubmed-meshheading:9873412-Tumor Cells, Cultured
|
pubmed:year |
1998
|
pubmed:articleTitle |
N3-methyl-mafosfamide as a chemically stable, alternative prodrug of mafosfamide.
|
pubmed:affiliation |
Department of Pharmaceutical Sciences, College of Pharmacy, St. John's University, Jamaica, New York 11439, USA. kmoon@mail.ncifcrf.gov
|
pubmed:publicationType |
Journal Article
|