Synthesis and cytotoxic activity of A-ring modified betulinic acid derivatives

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3137-40. doi: 10.1016/s0960-894x(03)00724-8.

Abstract

New A-ring modified betulinic acid derivatives having small steric hindrance were prepared and tested for cytotoxic activity on 3 cancer cell lines: 10 compounds showed stronger cytotoxic activity than betulinic acid. Especially, the compounds bearing 1-ene-3-oxo with electron-withdrawing groups at C2 showed strong cytotoxicity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / toxicity*
  • Betulinic Acid
  • Cell Line, Tumor
  • Humans
  • Pentacyclic Triterpenes
  • Triterpenes / chemical synthesis*
  • Triterpenes / toxicity*

Substances

  • Antineoplastic Agents
  • Pentacyclic Triterpenes
  • Triterpenes
  • Betulinic Acid