New Arteannuin B Derivatives and Their Cytotoxic Activity

Клочков, С. Г.; Neganova, Margarita E.; Pukhov, S. A.; Afanas’eva, S. V.; Aleksandrova, Yulia; Yandulova, Ekaterina

doi:10.1007/s10600-020-03059-2

Cited by 3 publications

(1 citation statement)

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“…An interesting object used for their modification can be natural origin products—sesquiterpene lactones, which contain activated double bonds in their structure and exhibit a wide range of biological activity. The antitumor potential of this class of compounds is confirmed by their ability to modulate a number of mechanisms involved in the development of oncological diseases, in particular, the processes associated with oxidative stress [ 14 , 15 , 16 ], the mitochondria functioning [ 17 ], and the glycolytic profile of transformed cells [ 18 , 19 ].…”

Section: Introductionmentioning

confidence: 99%

N-Alkylation of Anthracycline Antibiotics by Natural Sesquiterpene Lactones as a Way to Obtain Antitumor Agents with Reduced Side Effects

et al. 2021

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Anthracycline antitumor antibiotics are one of the promising classes of chemotherapeutic agents for cancer treatment. The main deterrent to their use is high toxicity to a healthy environment, including cumulative cardiotoxicity. In our work, bipharmacophore molecules containing in their structure a fragment of the known anthracycline antibiotics daunorubicin and doxorubicin and natural sesquiterpene lactones were obtained for the first time. When studying the biological activity of the synthesized compounds, it was found that with equal and, in some cases, higher cytotoxicity and glycolysis inhibition by anthracycline antibiotics conjugates with sesquiterpene lactones in comparison with doxo- and daunorubicin, a reduced damaging effect on the functioning of rat heart mitochondria was observed. The results obtained allow us to confirm the assumption that the chemical modification of the anthracycline antibiotics molecules doxo- and daunorubicin by natural sesquiterpene lactones can be a promising strategy for creating potential antitumor chemotherapeutic drugs with a pronounced cytotoxic effect on tumor cells and a reduced damaging effect on healthy cells of the human organism.

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