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

Research output: Contribution to journalArticle

Abstract

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.

Details

Authors
  • Henrik Sunden
  • Mareike C. Holland
  • Pekka K. Poutiainen
  • Tiina Jaaskelainen
  • Juha T. Pulkkinen
  • Jorma J. Palvimo
  • Roger Olsson
Organisations
Research areas and keywords

Subject classification (UKÄ) – MANDATORY

  • Medicinal Chemistry
Original languageEnglish
Pages (from-to)1569-1574
JournalJournal of Medicinal Chemistry
Volume58
Issue number3
Publication statusPublished - 2015
Publication categoryResearch
Peer-reviewedYes