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Novel 2-amino(substituted pyrimidin-2-yl)benzimidazole and 2-amino-3,4-dihydro[1,3,5]triazino[1,2- a ]benzimidazole hybrids were synthesized and evaluated for their  in vitro  antitumor activity at National Cancer Institute (NCI), against 60 human cell lines for primary anticancer screening. Among the tested compounds,  8  and  23  exhibited significant growth inhibition. Compound  8  was very promising anticancer; therefore, this compound passed on to further evaluation at five concentration levels (0.01–100 uM), and it showed potent activity in five-dose testing. Detailed synthesis, spectroscopic, and biological data are reported.

Synthesis and Antitumor Activity of Novel Hybrids of Pyrimidine/Benzimidazole Scaffolds