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Updated: Oct 2, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
N-Naphthoyl Thiourea Derivatives: An Efficient Ultrasonic-Assisted Synthesis, Reaction, and In Vitro Anticancer
Wael Abdelgayed Ahmed Arafa1, Amira Atef Ghoneim1, Asmaa K Mourad2
1Chemistry Department, College of Science, Jouf University, P. O. Box 2014, Sakaka 2014 Jouf, Kingdom of Saudi Arabia.
Abstract:
This work demonstrates the optimization of an efficient, mild, and environmentally friendly synthetic approach to access a diverse library of N-naphthoyl thioureas. These derivatives could be exploited as precursor scaffolds for designing valuable heterocycles with anticipated biological activities. Additionally, the utilization of a copper complex derived from the newly synthesized N-naphthoyl thiourea ligand in the photodegradation of methyl orange (MO) dye was explored. The antiproliferative effect of the synthesized derivatives was examined against MCF-7, HCT116, and A549 cancer cell lines. Most of the assembled derivatives revealed a significant cytotoxic effect, in some cases, greater than doxorubicin. Of these, the copper complex demonstrated significant antitumor activities (IC50 < 1.3 μM) and lesser cytotoxic impact (IC50 > 76 μM), indicating its possibility as a pioneering candidate for future carcinogenic pharmaceutics. Relations between the structure and activity also have been addressed.
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