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Updated: May 20, 2025
Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
1,2,3-Triazole Tethered Spiro[Indoline-Oxirane] Derivatives Induce Anticancer Effects in Human Hepatoma Cells
Shashikala Mariswamy Rajesh1, Prasanna Doddakunche Shivaramu2,3, Chandra Sekhar Bhol3
1Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysuru, India.
Abstract:
Epoxides are well-known compounds as anticancer agents. In this article, we present the synthesis of novel 3'-phenyl-1-((1-aryl-1H-1,2,3-triazol-5-yl)methyl)spiro[indoline-3,2'-oxiran]-2-one derivatives by the regioselective reaction of sulfur ylides with 1,2,3-triazole-tethered isatins and their anticancer effects on hepatocellular carcinoma (HCC) cells HepG2 and HCCLM3. The cell viability assays indicated that RR-01 and RR-07 had emerged as the most potent cytotoxic agents on the tested cell lines. Colony formation and migration assay results confirmed the anticancer effects of these compounds by inhibiting the formation of colonies and migration. Further, nuclear fragmentation staining assay showed that the compounds induce apoptosis. Acridine orange staining assays showed that our lead candidates (RR-01 and RR-07) induced autophagy in liver cancer cells.
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