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Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators

Schlienger, Nathalie ; Lund, Birgitte W. ; Pawlas, Jan ; Badalassi, Fabrizio ; Bertozzi, Fabio ; Lewinsky, Rasmus ; Fejzic, Alma ; Thygesen, Mikkel B. ; Tabatabaei, Ali and Bradley, Stefania Risso , et al. (2009) In Journal of Medicinal Chemistry 52(22). p.7186-7191
Abstract

Herein we describe the discovery of ACP-105 (1), a novel and potent nonsteroidal selective androgen receptor modulator (SARM) with partial agonist activity relative to the natural androgen testosterone. Compound 1 was developed from a series of compounds found in a HTS screen using the receptor selection and amplification technology (R-SAT). In vivo, 1 improved anabolic parameters in a 2-week chronic study in castrated male rats. In addition to compound 1, a number of potent antiandrogens were discovered from the same series of compounds whereof one compound, 13, had antagonist activity at the AR T877A mutant involved in prostate cancer.

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publishing date
type
Contribution to journal
publication status
published
in
Journal of Medicinal Chemistry
volume
52
issue
22
pages
7186 - 7191
publisher
The American Chemical Society (ACS)
external identifiers
  • pmid:19856921
  • scopus:70949086681
ISSN
0022-2623
DOI
10.1021/jm901149c
language
English
LU publication?
no
id
7441ceab-66e7-4152-8eda-642490f21af1
date added to LUP
2019-10-02 09:44:41
date last changed
2024-02-15 22:34:17
@article{7441ceab-66e7-4152-8eda-642490f21af1,
  abstract     = {{<p>Herein we describe the discovery of ACP-105 (1), a novel and potent nonsteroidal selective androgen receptor modulator (SARM) with partial agonist activity relative to the natural androgen testosterone. Compound 1 was developed from a series of compounds found in a HTS screen using the receptor selection and amplification technology (R-SAT). In vivo, 1 improved anabolic parameters in a 2-week chronic study in castrated male rats. In addition to compound 1, a number of potent antiandrogens were discovered from the same series of compounds whereof one compound, 13, had antagonist activity at the AR T877A mutant involved in prostate cancer.</p>}},
  author       = {{Schlienger, Nathalie and Lund, Birgitte W. and Pawlas, Jan and Badalassi, Fabrizio and Bertozzi, Fabio and Lewinsky, Rasmus and Fejzic, Alma and Thygesen, Mikkel B. and Tabatabaei, Ali and Bradley, Stefania Risso and Gardell, Luis R. and Piu, Fabrice and Olsson, Roger}},
  issn         = {{0022-2623}},
  language     = {{eng}},
  month        = {{10}},
  number       = {{22}},
  pages        = {{7186--7191}},
  publisher    = {{The American Chemical Society (ACS)}},
  series       = {{Journal of Medicinal Chemistry}},
  title        = {{Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators}},
  url          = {{http://dx.doi.org/10.1021/jm901149c}},
  doi          = {{10.1021/jm901149c}},
  volume       = {{52}},
  year         = {{2009}},
}