Novel Targeted Therapeutics for Castration Resistant Prostate Cancer

Abstract

Successful synthesis and purification of 5F02 analogs with different chemical properties. The effect of histone-dependent PARP-1 inhibitors on androgen-dependent and -independent activation of AR signaling was evaluated. The functional antitumor activity of 5F02 and its analogs was examined in androgen-dependent and castration-resistant PC cells. 5F02 and its analogs demonstrated superior antitumor activity compared with NAD-like clinically relevant PARP-1 inhibitors olaparib, veliparib, and rucaparib. Physicochemical and ADME properties of 5F02 and its analogs were examined.

Open PDF

Document Details

Document Type
Technical Report
Publication Date
Sep 01, 2019
Accession Number
AD1090530

Entities

People

  • Alexei Tulin

Organizations

  • University of North Dakota

Tags

DTIC Thesaurus Topics

  • Androgen Receptors
  • Androgens
  • Biomedical Research
  • Castration
  • Cell Line
  • Department Of Defense
  • Health Services
  • Inhibitors
  • Medical Personnel
  • Patent Applications
  • Professional Development
  • Prostate
  • Prostate Cancer
  • Students
  • Therapy
  • Toxicity
  • Training

Fields of Study

  • Biology
  • Chemistry

Readers

  • Oncology (Cancer Research).
  • Prostate Cancer Biology.