Abstract:
:We report the synthesis and a study of the structure-activity relationships of a new series of diarylhydrazides as potential selective non-ligand binding pocket androgen receptor antagonists. Their biological activity as antiandrogens in the context of the development of treatments for castration resistant prostate cancer was evaluated using in vitro time resolved fluorescence resonance energy transfer and fluorescence polarization on target assays. Additionally, a theoretical study combining docking and molecular dynamics methods was performed to provide insight into their mechanism of action as a basis for further lead optimization studies.
journal_name
J Chem Inf Modeljournal_title
Journal of chemical information and modelingauthors
Caboni L,Egan B,Kelly B,Blanco F,Fayne D,Meegan MJ,Lloyd DGdoi
10.1021/ci400189msubject
Has Abstractpub_date
2013-08-26 00:00:00pages
2116-30issue
8eissn
1549-9596issn
1549-960Xjournal_volume
53pub_type
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