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

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.