- Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators
-
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.
- Schlienger, Nathalie,Lund, Birgitte W.,Pawlas, Jan,Badalassi, Fabrizio,Bertozzi, Fabio,Lewinsky, Rasmus,Fejzic, Alma,Thygesen, Mikkel B.,Tabatabaei, Ali,Bradley, Stefania Risso,Gardell, Luis R.,Piu, Fabrice,Olsson, Roger
-
supporting information; experimental part
p. 7186 - 7191
(2010/07/04)
-
- Aminophenyl derivatives as selective androgen receptor modulators
-
Disclosed herein is a novel class of aminophenyl compounds having the structure: wherein R1 is cyano or nitro and ring A is a bi- or tricyclic bridged heterocycle and to their use as modulators of androgen receptor for the treatment or preventi
- -
-
Page/Page column 18
(2008/06/13)
-