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


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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).

About the authors

E. F. Khusnutdinova

Ufa Institute of Chemistry, Ufa Federal Research Center, Russian Academy of Sciences

Author for correspondence.
Email: ElmaH@inbox.ru
Russian Federation, Ufa, 450054

A. V. Petrova

Ufa Institute of Chemistry, Ufa Federal Research Center, Russian Academy of Sciences

Email: ElmaH@inbox.ru
Russian Federation, Ufa, 450054

O. B. Kazakova

Ufa Institute of Chemistry, Ufa Federal Research Center, Russian Academy of Sciences

Email: ElmaH@inbox.ru
Russian Federation, Ufa, 450054

A. E. Barmashov

Blokhin National Medical Research Center of Oncology, Ministry of Health, Russian Federation

Email: ElmaH@inbox.ru
Russian Federation, Moscow, 115478


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