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Synthesis and Cytotoxicity of Triterpenic Acids Modified at C3 and C28 Positions

Abstract

Series of N-, S- and Br-derivatives of betulinic, oleanolic, and ursolic acids have been synthesized and screened for their in vitro antitumor activity (cytotoxicity). N-Methylpiperazinylamide of 2-[3-pyridinylidene]-ursolic acid and methyl 2-methylideneureido-betulonate have shown significant cytotoxic activity against the PC3 cancer cells (IC50 = 8 μM) and HCT-116 cell line (IC50 = 5.7 μM).

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Correspondence to E. F. Khusnutdinova.

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This article does not contain any studies with the use of animals or humans as research subjects.

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The authors state that there are no conflict of interests.

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Translated by A. Levina

Corresponding author: fax: +7 (347) 235-60-66; e-mail: ElmaH@inbox.ru.

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Khusnutdinova, E.F., Petrova, A.V., Kazakova, O.B. et al. Synthesis and Cytotoxicity of Triterpenic Acids Modified at C3 and C28 Positions. Russ J Bioorg Chem 45, 552–557 (2019) doi:10.1134/S1068162019050042

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Keywords:

  • triterpenoids, oleanolic
  • ursolic, betulinic acids, synthesis, cytotoxiсity