Synthesis of conjugates of sesquiterpene lactones with 3,5-bis(arylidene)piperidin-4-ones as potential NF-κB modulators using phase transfer catalysis conditions

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发表日期：

2024年11月1日

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O. I. Artyushin,
E. V. Sharova,
E. V. Smirnova,
A. V. Semakov,
Yu. R. Aleksandrova,
M. E. Neganova,
V. K. Brel

摘要

A simple method for modifying sesquiterpene lactones with 3,5-bis(arylidene)piperi-din-4-ones using the phase-transfer catalytic aza-Michael addition in the MeCN—K₂CO₃ system was developed. Molecular docking revealed that the synthesized conjugates of isoalantolactone, alantolactone, and dehydrocostus lactone with various bis(arylidene)-piperidones directly interact with the DNA binding site of the p50 subunit of nuclear factor κB, which may be indicative of their ability to induce apoptotic death of the tumor cells due to activation of the death receptor expression and, thereby, to exhibit an antitumor effect.