Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
5
pubmed:dateCreated
2010-6-3
pubmed:abstractText
A series of mifepristone derivatives with different "linker groups" in position 4' of the phenyl ring in the 11beta-position of the steroid scaffold (2-41) have been synthesized. Their antigestagenic activites were determined in a cell-based assay (alkali phosphatase assay in T47-D breast cancer cells) and compared with that of the parent compound mifepristone. SAR and QSAR studies reveal the influence of both lipophilicity and partial charge based van der Waals surface area descriptors on biological activity. Within the series of compounds described in this study, three mifepristone derivatives are identified with considerably high antigestagenic activity. These compounds are regarded as useful starting materials for the synthesis of either physiologically stable or cleavable progesterone receptor-binding conjugates for therapeutic or diagnostic purposes.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Mar
pubmed:issn
1520-4804
pubmed:author
pubmed:issnType
Electronic
pubmed:day
12
pubmed:volume
52
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1268-74
pubmed:meshHeading
pubmed:year
2009
pubmed:articleTitle
Syntheses and antigestagenic activity of mifepristone derivatives.
pubmed:affiliation
Department of Pharmaceutical Chemistry-Medicinal Chemistry, Institute of Pharmaceutical Sciences, University of Graz, Graz, Austria.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't