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Synthesis and Biological Evaluation of Second-Generation Tropanol-Based Androgen Receptor Modulators

Sunden, Henrik ; Holland, Mareike C. ; Poutiainen, Pekka K. ; Jaaskelainen, Tiina ; Pulkkinen, Juha T. ; Palvimo, Jorma J. and Olsson, Roger LU (2015) In Journal of Medicinal Chemistry 58(3). p.1569-1574
Abstract
To circumvent antiandrogen resistance in prostate cancer, antiandrogens effective for both the androgen receptor (AR) and AR mutants are required. The AR antagonists in this study originate from previous findings, which showed that subtle differences in substitution pattern lead to a conformational change that alters the ligand activity, rendering an agonist to an antagonist. We have identified small yet potent tropanol-based ligands possessing significant antiandrogenic activity with both wild-type AR and the two most common AR ligand binding domain (LBD) mutants.
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Journal of Medicinal Chemistry
volume
58
issue
3
pages
1569 - 1574
publisher
The American Chemical Society (ACS)
external identifiers
  • wos:000349573800045
  • scopus:84922824050
  • pmid:25646649
ISSN
1520-4804
DOI
10.1021/jm501995n
language
English
LU publication?
yes
id
1f28a95d-9977-4d08-a04a-60b50d088b85 (old id 5173008)
date added to LUP
2016-04-01 11:08:20
date last changed
2020-01-12 07:18:28
@article{1f28a95d-9977-4d08-a04a-60b50d088b85,
  abstract     = {To circumvent antiandrogen resistance in prostate cancer, antiandrogens effective for both the androgen receptor (AR) and AR mutants are required. The AR antagonists in this study originate from previous findings, which showed that subtle differences in substitution pattern lead to a conformational change that alters the ligand activity, rendering an agonist to an antagonist. We have identified small yet potent tropanol-based ligands possessing significant antiandrogenic activity with both wild-type AR and the two most common AR ligand binding domain (LBD) mutants.},
  author       = {Sunden, Henrik and Holland, Mareike C. and Poutiainen, Pekka K. and Jaaskelainen, Tiina and Pulkkinen, Juha T. and Palvimo, Jorma J. and Olsson, Roger},
  issn         = {1520-4804},
  language     = {eng},
  number       = {3},
  pages        = {1569--1574},
  publisher    = {The American Chemical Society (ACS)},
  series       = {Journal of Medicinal Chemistry},
  title        = {Synthesis and Biological Evaluation of Second-Generation Tropanol-Based Androgen Receptor Modulators},
  url          = {http://dx.doi.org/10.1021/jm501995n},
  doi          = {10.1021/jm501995n},
  volume       = {58},
  year         = {2015},
}