Synthesis and antitumor activity of 5,6-dihydro-17-hydroxy icogenin analogs

Eur J Med Chem. 2012 May:51:200-5. doi: 10.1016/j.ejmech.2012.02.043. Epub 2012 Mar 2.

Abstract

Four 5,6-dihydro-17-hydroxy icogenin analogs were designed and synthesized. Their in vitro antitumor activities were tested by the standard MTT assay. Compound 22 (IC(50) = 3.38-8.30 μM) and compound 23 (IC(50) = 1.90-9.69 μM) showed potential antitumor activities against the entire tested seven cancer cell lines. The SAR (structure activity relationship) research showed that the introduction of 17-hydroxy lowered the antitumor activity to an extent.

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Chemistry Techniques, Synthetic
  • Drug Design
  • Humans
  • Saponins / chemical synthesis*
  • Saponins / chemistry
  • Saponins / pharmacology*
  • Steroids / chemical synthesis*
  • Steroids / chemistry
  • Steroids / pharmacology*

Substances

  • 5,6-dihydro-17-hydroxy icogenin
  • Antineoplastic Agents
  • Icogenin
  • Saponins
  • Steroids