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Updated: Apr 17, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and anticancer activities of ceritinib analogs modified in the terminal piperidine ring
Peng Wang1, Jin Cai2, Junqing Chen2
1Department of Biomedical Engineering, School of Engineering, China Pharmaceutical University, Nanjing 210009, China; School of Biological Science & Medical Engineering, Southeast University, Nanjing 210096, China.
Abstract:
A series of new ceritinib analogs by extensive functionalization of the tail piperidine ring with various phosphamides and carbamates have been synthesized. All the ceritinib derivatives were evaluated for their cytotoxic activities against H2228 cell line. From the activity profile obtained, three of the tested compounds (compounds 4, 7 and 9) showed significant cytotoxic effects. Among these derivatives compound 9 was found to possess cytotoxicity that is better than standard drug ceritinib (IC50 = 24 nM). Moreover, compound 9 demonstrated robust tumor growth inhibition in vivo model.
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