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Updated: Jun 27, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and biological evaluation of novel 2,4,5-substituted pyrimidine derivatives for anticancer activity
Fuchun Xie1, Hongbing Zhao, Lizhi Zhao
1Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Medicinal Chemistry, Shanghai, China.
Abstract:
A series of novel 2,4,5-substituted pyrimidine derivatives were synthesized and evaluated for inhibition against the human hepatocellular carcinoma BEL-7402 cancer cell line. Several compounds showed potent inhibition with an IC(50) value less than 0.10 microM. Structure-activity relationships for this class of compounds at the 2- and 5-position of the pyrimidine scaffold have been elucidated. The most active compound 7gc showed good inhibition of several different human cancer cell lines with IC(50) values from 0.024 to 0.55 microM.
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