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 IC50 value less than 0.10 μM. 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 ...