beta-Alkylthio indolyl carbinols: potent nonsteroidal antiandrogens with oral efficacy in a prostate cancer model

Bioorg Med Chem Lett. 2007 May 1;17(9):2545-8. doi: 10.1016/j.bmcl.2007.02.014. Epub 2007 Feb 8.

Abstract

Through an in vivo screening model, we developed the in vivo SAR of beta-alkylthio indolyl carbinols. Through these efforts we identified a compound with potent oral in vivo efficacy in both immature and mature rat prostate weight reduction models and in a murine xenograft prostate cancer model.

MeSH terms

  • Administration, Oral
  • Androgen Antagonists / chemical synthesis*
  • Androgen Antagonists / pharmacology*
  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / chemical synthesis*
  • Chemistry, Pharmaceutical / methods*
  • Disease Models, Animal
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Indoles / chemical synthesis*
  • Indoles / pharmacology
  • Male
  • Methanol / analogs & derivatives*
  • Methanol / chemistry*
  • Mice
  • Neoplasm Transplantation
  • Prostatic Neoplasms / drug therapy*
  • Rats
  • Structure-Activity Relationship

Substances

  • Androgen Antagonists
  • Antineoplastic Agents
  • Indoles
  • Methanol