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Synthesis and Biological Evaluation of Second-Generation Tropanol-Based Androgen Receptor Modulators

Henrik Sundén ; Mareike C. Holland ; P. K. Poutiainen ; T. Jaaskelainen ; J. T. Pulkkinen ; J. J. Palvimo ; Roger Olsson
Journal of Medicinal Chemistry (0022-2623). Vol. 58 (2015), 3, p. 1569-1574.
[Artikel, refereegranskad vetenskaplig]

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.

Nyckelord: RESISTANT PROSTATE-CANCER, ANTIANDROGEN RESISTANCE, ANTI-ANDROGENS, BETA-AGONIST, DESIGN, ANTAGONISTS, POTENT, IDENTIFICATION, DISCOVERY, SERIES, Chemistry, Medicinal



Denna post skapades 2015-03-16. Senast ändrad 2017-09-14.
CPL Pubid: 213836

 

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Institutioner (Chalmers)

Institutionen för kemi och molekylärbiologi (GU)

Ämnesområden

Kemi

Chalmers infrastruktur