New steroidal dimers with antifungal and antiproliferative activity

J Med Chem. 2004 Mar 11;47(6):1591-4. doi: 10.1021/jm030376y.

Abstract

Bile acid-derived novel amphiphilic topology was designed and synthesized in the form of steroidal dimers. These dimers were tested for antifungal and antiproliferative activity in vitro. N(1),N(3)-Diethylenetriaminebis[cholic acid amide] was found to be active against C. albicans, Y. lipolytica, and B. poitrassi at nanomolar concentration and did not show any effect on cell proliferation. N(1),N(2)-Ethylenediaminebis[deoxycholic acid amide] totally inhibited the growth of human oral cancer (HEp-2) and human breast cancer (MCF-7) cells.

MeSH terms

  • Antifungal Agents / chemical synthesis*
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Bile Acids and Salts / chemistry*
  • Candida albicans / drug effects
  • Candida albicans / isolation & purification
  • Cell Division / drug effects
  • Cell Line
  • Cell Line, Tumor
  • Dimerization
  • Drug Screening Assays, Antitumor
  • Fungi / drug effects
  • Humans
  • Steroids / chemical synthesis*
  • Steroids / chemistry
  • Steroids / pharmacology
  • Structure-Activity Relationship
  • Yarrowia / drug effects

Substances

  • Antifungal Agents
  • Antineoplastic Agents
  • Bile Acids and Salts
  • Steroids