Synthesis and Biological Evaluation of Second-Generation Tropanol-Based Androgen Receptor Modulators
(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.
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/5173008
- author
- Sunden, Henrik
; Holland, Mareike C.
; Poutiainen, Pekka K.
; Jaaskelainen, Tiina
; Pulkkinen, Juha T.
; Palvimo, Jorma J.
and Olsson, Roger
LU
- organization
- publishing date
- 2015
- 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
- 2022-05-18 08:42:16
@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}}, }