New Arteannuin B Derivatives and Their Cytotoxic Activity
2020
Klochkov, S. G. | Neganova, M. E. | Pukhov, S. A. | Afanas’eva, S. V. | Aleksandrova, Yu. R. | Yandulova, E. Yu
Previously unknown conjugates of the natural sesquiterpene lactone arteannuin B, which was isolated from Artemisia annua, were synthesized via Michael reactions with pharmacophoric amines and tested in vitro for cytotoxic activity. The compounds were shown to exhibit antiproliferative properties for various tumor cell lines. The most active derivatives had IC₅₀ values of 8–36 μM, which exceeded that of starting arteannuin B. Practically all obtained conjugates were found to modulate glycolysis in MCF7 tumor cells. The lead compound was the conjugate with 3-ethoxycarbonylpiperidine, which could be considered a platform for developing antitumor drugs.
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