Synthesis and antitumor activity of N-acylhydrazones from betulin diacetate

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Abstract

Eight new N -acylhydrazones were synthesized from betulin diacetate by its low-temperature ozonolysis to obtain 3β,3,28-diacetoxyoxy-20-oxo-29-norlupan and condensation of the latter with hydrazides of aliphatic and aromatic acids. Cytotoxic activity of the obtained compounds in relation to a number of tumor cells was studied in vitro . Derivatives obtained by condensation of 3β,3,28-diacetoxy-20-oxo-29-norlupan with hydrazides of salicylic, isonicotinic and nicotinic acids showed moderate activity against cell lines of human hepatocellular carcinoma HepG2, human colon cancer HTC-116, leukemia THP-1, acute T-cell leukemia Jurkat.

About the authors

Yu. V. Myasoyedova

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

Email: ern_lbrn@bk.ru

E. R Belyaeva

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

Email: ern_lbrn@bk.ru

N. M Ishmuratova

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

Email: ern_lbrn@bk.ru

D. V Ishmetova

Institute of Biochemistry and Genetics, Ufa Federal Research Center, Russian Academy of Sciences

Email: ern_lbrn@bk.ru

V. A Vakhitov

Institute of Biochemistry and Genetics, Ufa Federal Research Center, Russian Academy of Sciences

Email: ern_lbrn@bk.ru

G. Yu. Ishmuratov

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

Email: ern_lbrn@bk.ru

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