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

Abstract

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.

Keywords:

• Anticancer activity
• hybrid
• NCI
• pyrimidine/benzimidazole
• s-triazino[1,2- a]benzimidazole
• synthesis

Acknowledgments

We are grateful to the authority of National Cancer Institute (Bethesda, Maryland, USA) for carrying out the in vitro anticancer screening.