rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
2
|
pubmed:dateCreated |
2004-12-17
|
pubmed:abstractText |
A novel series of isoindoledione based compounds were identified as potent antagonists of the androgen receptor (AR). SAR around this series revealed dramatic differences in binding and function in mutant variants (MT) of the AR as compared to the wild type (WT) receptor. Optimization of the aniline portion revealed substitution patterns, which yielded potent antagonist activity against the WT AR as well as the MT AR found in the LNCaP and PCa2b human prostate tumor cell lines.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Jan
|
pubmed:issn |
0960-894X
|
pubmed:author |
pubmed-author:AttarRicardo MRM,
pubmed-author:BalogAaronA,
pubmed-author:GengJiepingJ,
pubmed-author:GottardisMarco MMM,
pubmed-author:HuntJohn TJT,
pubmed-author:MartinezRogelioR,
pubmed-author:PickeringDaciaD,
pubmed-author:RizzoCheryl ACA,
pubmed-author:SalvatiMark EME,
pubmed-author:WeiDonna DDD,
pubmed-author:WeinmannRobertoR
|
pubmed:issnType |
Print
|
pubmed:day |
17
|
pubmed:volume |
15
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
389-93
|
pubmed:dateRevised |
2010-11-18
|
pubmed:meshHeading |
pubmed-meshheading:15603960-Androgen Antagonists,
pubmed-meshheading:15603960-Androgen Receptor Antagonists,
pubmed-meshheading:15603960-Animals,
pubmed-meshheading:15603960-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:15603960-Humans,
pubmed-meshheading:15603960-Indoles,
pubmed-meshheading:15603960-Inhibitory Concentration 50,
pubmed-meshheading:15603960-Male,
pubmed-meshheading:15603960-Mutation,
pubmed-meshheading:15603960-Prostatic Neoplasms,
pubmed-meshheading:15603960-Receptors, Androgen,
pubmed-meshheading:15603960-Structure-Activity Relationship,
pubmed-meshheading:15603960-Tumor Cells, Cultured
|
pubmed:year |
2005
|
pubmed:articleTitle |
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.
|
pubmed:affiliation |
Department of Oncology Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. mark.salvati@bms.com
|
pubmed:publicationType |
Journal Article,
Comparative Study
|