Synthesis and antiproliferative activity of 17-[1',2',3']-selenadiazolylpregnenolone compounds

Steroids. 2018 Dec:140:151-158. doi: 10.1016/j.steroids.2018.10.004. Epub 2018 Oct 6.

Abstract

Using pregnenolone as a starting material, some 3-substituted 17-[1',2',3']-selenadiazolylpregnenolone derivatives were synthesized, and their structures were characterized by IR, NMR and HRMS. The in vitro antitumor activity of the compounds was assayed against PC-3、SKOV3、T47D、MCF-7 and HEK293T cell lines. The results show that some compounds display selective antiproliferative activity against PC-3 and SKOV3 cells lines and are almost inactive to normal kidney epithelial cells (HEK293T). The IC50 value are much better than that of abiraterone (positive control).

Keywords: 17-[1′,2′,3′]-Selenadiazolylpregnenolone; Antiproliferative activity; Organoselenium compounds; Pregnenolone; [1′,2′,3′]-Selenadiazole.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Chemistry Techniques, Synthetic
  • Drug Screening Assays, Antitumor
  • Humans
  • Organoselenium Compounds / chemical synthesis*
  • Organoselenium Compounds / chemistry
  • Organoselenium Compounds / pharmacology*
  • Pregnenolone / chemistry*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Organoselenium Compounds
  • Pregnenolone