[Antitumor activity of dihydrobetulonic acid amides in vitro and in vivo]

Bioorg Khim. 2013 Mar-Apr;39(2):221-9. doi: 10.1134/s106816201302012x.
[Article in Russian]

Abstract

Amides with homopiperidinic and piperazinic cycles were synthesized from dihydrobetulonic acid which was obtained by dihydrobetulin oxidation. All substances have shown high antitumor activity (CCID50 3.5-36.2 microM) in vitro in lymphoid (CEM-13, U-937) and monocytic (MT-4) human cell lines. Amides with methyl- and ethyl-piperazinic residues don't influence viability of Lung Lewis Carcinoma cell in culture and haven't any significant effect to its transplantates in C57BL/6 mice. But such amides inhibit efficiently the metastatic elaboration in lung of these mice. The antimetastatic activity increases followed by the change of aliphatic residue length in piperazinic cycle from methyl to ethyl.

Publication types

  • English Abstract

MeSH terms

  • Amides / chemical synthesis*
  • Amides / chemistry
  • Amides / pharmacology
  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Carcinoma, Lewis Lung / drug therapy
  • Carcinoma, Lewis Lung / pathology
  • Cell Line, Tumor
  • Cell Survival / drug effects*
  • Humans
  • Lung Neoplasms / drug therapy
  • Lung Neoplasms / pathology
  • Lung Neoplasms / secondary
  • Mice
  • Oleanolic Acid / analogs & derivatives*
  • Oleanolic Acid / chemical synthesis
  • Oleanolic Acid / chemistry
  • Oleanolic Acid / pharmacology

Substances

  • Amides
  • Antineoplastic Agents
  • betulonic acid
  • Oleanolic Acid