Synthesis and anti-inflammatory, cytotoxic activity of heteroatomic derivatives of estafiatine

Abstract

Amination reactions of guaianolide of estafiatine were investigated in this article. It is shown that secondary amines interact only with the conjugated exomethylene bond of the lactone cycle with the formation of Michael adducts. Discussed in this paper sesquiterpene lactone estafiatine (1) and its modified derivatives were studied in order to obtain new biologically active compounds and to determine of influence of structural features of the molecules of this series on their biological activity. It is found that the number of synthesized nitrogen- containing derivatives of estafiatine have anti-inflammatory and cytotoxic activity.