Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators
(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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- author
- publishing date
- 2009-10-26
- 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
- 2024-08-07 07:21:28
@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}}, }