6-hydroximino-4-aza-A-homo-cholest-3-one and related analogue as a potent inducer of apoptosis in cancer cells

Steroids. 2012 Jul;77(8-9):829-34. doi: 10.1016/j.steroids.2012.04.016. Epub 2012 Apr 23.

Abstract

Here we report that 6-hydroximino-4-aza-A-homo-cholest-3-one and 6-hydroxyl-4-aza-A-homo-cholest-3-one, new steroidal lactams were synthesized recently, displayed antiproliferative activity against some cancer cells through inducing cancer cell apoptosis by activation of the intrinsic pathway. The apoptotic function of the compounds was demonstrated by release of cytochrome C, activation of caspase 3 and annexin V labeling. Furthermore, the compound was able to inhibit tumor growth in an athymic mouse model.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Annexin A5 / metabolism
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use*
  • Apoptosis / drug effects*
  • Blotting, Western
  • Caspase 3 / metabolism
  • Cell Proliferation / drug effects
  • Cytochromes c / metabolism
  • HT29 Cells
  • Humans
  • Lactams / chemistry
  • Lactams / pharmacology*
  • Lactams / therapeutic use*
  • Mice
  • Mice, Nude
  • Steroids / chemistry
  • Steroids / pharmacology*
  • Steroids / therapeutic use*

Substances

  • Annexin A5
  • Antineoplastic Agents
  • Lactams
  • Steroids
  • Cytochromes c
  • Caspase 3