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

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Author

  • Henrik Sunden
  • Mareike C. Holland
  • Pekka K. Poutiainen
  • Tiina Jaaskelainen
  • Juha T. Pulkkinen
  • Jorma J. Palvimo
  • Roger Olsson

Summary, in English

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.

Publishing year

2015

Language

English

Pages

1569-1574

Publication/Series

Journal of Medicinal Chemistry

Volume

58

Issue

3

Document type

Journal article

Publisher

The American Chemical Society (ACS)

Topic

  • Medicinal Chemistry

Status

Published

Research group

  • Chemical Biology and Therapeutics

ISBN/ISSN/Other

  • ISSN: 1520-4804