Synthesis and Biological Evaluation of Second-Generation Tropanol-Based Androgen Receptor Modulators
Artikel i vetenskaplig tidskrift, 2015
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.
DESIGN
RESISTANT PROSTATE-CANCER
BETA-AGONIST
POTENT
SERIES
Chemistry
ANTIANDROGEN RESISTANCE
IDENTIFICATION
DISCOVERY
Medicinal
ANTAGONISTS
ANTI-ANDROGENS
Författare
Henrik Sundén
Göteborgs universitet
Mareike C. Holland
Göteborgs universitet
P. K. Poutiainen
T. Jaaskelainen
J. T. Pulkkinen
J. J. Palvimo
Roger Olsson
Göteborgs universitet
Journal of Medicinal Chemistry
0022-2623 (ISSN) 1520-4804 (eISSN)
Vol. 58 3 1569-1574Ämneskategorier
Kemi
DOI
10.1021/jm501995n