Synthesis of betulinic acid derivatives with activity against human melanoma

Bioorg Med Chem Lett. 1998 Jul 7;8(13):1707-12. doi: 10.1016/s0960-894x(98)00295-9.


Betulinic acid has been modified at C-3, C-20, and C-28 positions and the toxicity of the derivatives has been evaluated against cultured human melanoma (MEL-2) and human epidermoid carcinoma of the mouth (KB) cell lines. This preliminary investigation demonstrates that simple modifications of the parent structure of betulinic acid can produce potentially important derivatives, which may be developed as antitumor drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Betulinic Acid
  • Carcinoma, Squamous Cell / pathology
  • Drug Screening Assays, Antitumor
  • Humans
  • Hydrogen Bonding
  • Melanoma / pathology*
  • Mouth Neoplasms / pathology
  • Pentacyclic Triterpenes
  • Triterpenes / chemical synthesis*
  • Triterpenes / chemistry
  • Triterpenes / pharmacology*


  • Antineoplastic Agents
  • Pentacyclic Triterpenes
  • Triterpenes
  • Betulinic Acid