Synthesis and antitumor activity of <i>N</i>-acylhydrazones from betulin diacetate

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.