Synthesis and Cytotoxic Activity of Azepane Derivatives Based on 2-Oxo-Allobetulin and Methyl 2-Oxo-Oleanoate

Objective: Triterpene lactams and azepanes were synthesized using 2-oxo-allobetulin oxime and methyl 2-oxo-oleanoate oxime. Methods: The cytotoxic activity of the synthesized compounds was studied in vitro on 60 tumor cell lines from nine different types of human cancer. Results and Discussion: C2-Azepano-allobetulin was shown to be active against leukemia, non-small cell lung cancer, and colon cancer cell lines, while C2-azepano-erythrodiol exhibited high activity (GI50 1.16–16.80 μM) against all studied cell lines, with the compound’s activity exceeding that of the reference drug, 5-fluorouracil, against 14 cell lines. Conclusions: The high cytotoxic activity of the synthesized compounds demonstrates their potential as new antitumor agent candidates and justifies further study of their selectivity, as well as of their pharmacokinetic and toxicological profiles, to expand the possibilities for developing pharmacologically relevant agents based on 2-oxo-triterpenoids.