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  • Title: Synthesis and Cytotoxic Activity of Azine Derivatives of 6-Hydroxyxanthanodiene.
    Author: Neganova ME, Klochkov SG, Pukhov SA, Afanasieva SV, Aleksandrova YR, Yandulova EY, Avila-Rodriguez MF, Mikhaleva LM, Nikolenko VN, Somasundaram SG, Kirkland CE, Aliev G.
    Journal: Curr Cancer Drug Targets; 2020; 20(9):666-674. PubMed ID: 32316892.
    Abstract:
    BACKGROUND: The conjugates of the sesquiterpene lactone of the eremophilane series of 6- hydroxyxanthanodiene with hydrogenated azines (piperidines and piperazines) have been synthesized and identified by NMR spectrometer. OBJECTIVE: A lactone with an unusual skeleton "6-hydroxyxanthanodiene" was extracted from the plant Elecampane (Inula helenium L) and identified various species with NMR spectrometer. METHODS: The cytotoxic, mitochondrial, and antioxidant activities on different tumor lines such as A549, HCT116, RD and Jurkat were investigated and determined possible mechanisms. RESULTS: The results showed that the most potent compound was IIIi exhibiting highest cytotoxicity against RD cells (IC50 25.23 ± 0.04 μM), depolarized the mitochondrial membrane and was an effective antioxidant (IC50 inhibition of LP 10.68 ± 3.21 μM) without any toxic side effect on healthy cells. CONCLUSION: The conjugates of sesquiterpene lactone 6-hydroxyxanthanodiene III and hydrogenated azines may help to design potential promising anticancer drugs.
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