Androgen Receptor Antagonists and Anti-prostate Cancer Activities of Some Synthesized Steroidal Candidates

スポンサーリンク

概要

• 論文の詳細を見る

• In continuation of our previous work, a novel series of steroid derivatives were synthesized and their androgen receptor (AR) antagonist activities and in vivo antiandrogenic properties were evaluated. Twenty-one heterocyclic derivatives containing a cyanopyrane ring fused to a steroidal moiety were conveniently synthesized and screened for their antagonistic, antiandrogen and prostate anticancer activities comparable to that of bicalutamide as the reference control. Some of the compounds exhibited better antagonistic, antiandrogen and prostate anticancer activities than the reference controls. Initially the acute toxicity of the compounds was assayed via the determination of their LD50. Synthetic steroidal structures fused to a substituted cyanopyrane ring seem to be a promising approach in the search for novel leads for potent antagonistic, antiandrogen and prostate anticancer agents.

著者

• Bahashwan Saleh

  Department of Pharmacy, College of Health Science, Taibah University

• Al-Omar Mohamed

  Pharmaceutical Chemistry Department, College of Pharmacy, King Saud University

• Ezzeldin Essam

  Drug Bioavailability Laboratory, College of Pharmacy, King Saud University

• Abdalla Mohamed

  Research Unit, Univet Pharmaceutical Co.

• Fayed Ahmed

  Department of Pharmacy, College of Health Science, Taibah University

• Amr Abdel-Galil

  Drug Exploration & Development Chair (DEDC), College of Pharmacy, King Saud University

関連論文

• Androgen Receptor Antagonists and Anti-prostate Cancer Activities of Some Synthesized Steroidal Candidates
• Synthesis, Molecular Modeling, and Biological Evaluation of Novel Benzimidazole Derivatives as Inhibitors of Hepatitis C Virus RNA Replication

スポンサーリンク