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Updated: Jun 12, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Ultrasonic-assisted synthesis and antitumor evaluation of novel variant heterocyclic compounds based on piperidine
Asmaa Aboelnaga1, Eman El-Sayed Ebead1, Ekhlass Nassar1
1Chemistry Department, Faculty of Women for Arts, Science & Education, Ain Shams University, Heliopolis, Egypt.
Abstract:
Aim: This work explores the eco-friendly synthesis of various heterocycles from a piperidine-based compound (1) and explore their potential as antitumor agents.Materials & methods: Ultrasonic irradiation was used to synthesize heterocycles like pyridone, thiophene and coumarin, with computational tools analyzing stability and biological interactions.Results: Compounds 9 and 14 exhibit strong cytotoxic activity, surpassing doxorubicin. Compounds 2, 6, 10 and 13 exhibited intermediate activity, while compounds 3, 7 and 12 had minimal effects. Docking studies suggest potential ADORA1 receptor interaction. Computational tools analyze stability and interaction with biological systems, revealing potential antitumor mechanisms.Conclusion: Green synthesis of diverse heterocycles yielded potent antitumor agents (compounds 9 & 14). DFT and Docking studies suggest interaction with ADORA1 receptor, a potential mechanism.
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