Journal of Clinical & Experimental Pharmacology

Stein CY

Publications

• Research Article
  Elucidation of the Multiple Activities of Abiraterone by a Synthetic Chemistry Approach
  Author(s): Miaoling He, Ben Yi Tew, Stein CY, Darryl Rideout, Sumanta K Pal and Jeremy O JonesMiaoling He, Ben Yi Tew, Stein CY, Darryl Rideout, Sumanta K Pal and Jeremy O Jones
  
  Objective: Novel agents to treat metastatic prostate cancer include a class of drugs which function primarily by inhibiting the action of the CYP17 enzyme, which results in decreased androgen synthesis. Abiraterone and related molecules have been shown to decrease expression of the androgen receptor (AR) and to inhibit its transcriptional activity in addition to CYP17 inhibition. The structure-activity relationships (SAR) governing AR down regulation are less well understood than CYP17 and AR inhibition, so we designed abiraterone derivatives with the goal of better understanding the SAR of AR down regulation. Methods: We synthesized 17 abiraterone derivatives with unsaturated, cyclic and acyclic substituents containing hydrogen bond acceptors at C16 and C17 positions. We examined the ability of these compounds to inhibit CYP17 and AR, and to d.. View More»
  DOI: 10.4172/2161-1459.1000173

  Abstract PDF