Russian Journal of Bioorganic Chemistry

, Volume 41, Issue 3, pp 305–314 | Cite as

Synthesis and the antineoplastic activity of imidazolides of betulonic acid

  • O. B. Kazakova
  • N. I. Medvedeva
  • T. V. Lopatina
  • G. N. Apryshko
  • R. B. Pugacheva
  • N. P. Yavorskaya
  • I. S. Golubeva
  • G. A. Tolstikov


Lupane C-28-imidazolides containing 3-oxo-, 3-hydroxyimino-, and 2-cyano-2,3-seco-4(23)-ene fragments in cycle A have been synthesized. 3-3-Hydroxyimino-lup-20(29)-en-28-yl-1H-imidazole-1-carboxylate showed the highest antineoplastic activity in experiments in vitro, significantly inhibiting the growth and inducing the death of cells of lung, colon cancer, breast, central nervous system, ovarian, prostate, renal, leukemia, and melanoma cancers. In experiments on mice, it had a moderate antineoplastic effect on inoculated breast adenocarcinoma Ca755 and large intestine adenocarcinoma AKATOL.


lupane triterpenoids betulonic acid imidazolides antineoplastic activity 


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Copyright information

© Pleiades Publishing, Ltd. 2015

Authors and Affiliations

  • O. B. Kazakova
    • 1
  • N. I. Medvedeva
    • 1
  • T. V. Lopatina
    • 1
  • G. N. Apryshko
    • 2
  • R. B. Pugacheva
    • 2
  • N. P. Yavorskaya
    • 2
  • I. S. Golubeva
    • 2
  • G. A. Tolstikov
    • 1
  1. 1.Institute of Organic Chemistry, Ufa Scientific CenterRussian Academy of SciencesUfaRussia
  2. 2.Blokhin Russian Oncological Research CenterMoscowRussia

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