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Article

Synthesis and biological evaluation of second-generation tropanol-based androgen receptor modulators.

Journal of medicinal chemistry - 12 Feb 2015

Sundén Henrik, Holland Mareike C, Poutiainen Pekka K, Jääskeläinen Tiina, Pulkkinen Juha T, Palvimo Jorma J, Olsson Roger

Abstract excerpt

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...

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Identifiers

PMID: 25646649
DOI: 10.1021/jm501995n

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026. Manifest publication-graph-cohort-2026-09-05.1.

Source receipt: pubmed, retrieved 5 Sept 2026.

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