Ontology highlight
ABSTRACT:
SUBMITTER: Pepe A
PROVIDER: S-EPMC7581280 | biostudies-literature | 2013 Nov
REPOSITORIES: biostudies-literature
Pepe Antonella A Pamment Michael M Kim Yeong Sang YS Lee Sunmin S Lee Min-Jung MJ Beebe Kristin K Filikov Anton A Neckers Len L Trepel Jane B JB Malhotra Sanjay V SV
Journal of medicinal chemistry 20131030 21
A library of 3-hydroxy-2,3-dihydropyridones was synthesized, and their activities as antiandrogens were tested in the human prostate cancer cell line LNCaP. Structure-activity relationship (SAR) studies resulted in the identification of a potent compound whose activity is comparable to that of MDV3100. Homology modeling and molecular mechanics were used to build a structural model of the androgen receptor-ligand binding domain and to investigate the structural basis of the antagonism. The model ...[more]