A. Mulugeta, G. Medhin, G. Yimer
Dec 7, 2016
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Open Access Journal of Clinical Trials
Abstract
I medicinal chemistry, purine motifs have attracted a great deal of research interest due to their preponderance in pharmaceutically indispensable compounds. Substituted purine especially 2, 6-disubstituted purine known to be very important medicinal and pharmaceutical intermediate. benzimidazoles are categorized in the important pharmacophores and privileged sub-structures in medicinal chemistry owing to their involvement as a key component for various biological activities. Therefore, introduction of benzimidazole at C-6 position of 2, 6-dichloropurine is supposed to improve its activity and thereby selectivity. Due to individual importance of purine and benzimidazole in living cells, we will present their synthesis as hybrids of benzimidazole at 6-position of purine and evaluated in vitro anticancer activities. Thus, a series of purine/benzimidazole hybrids were prepared by introduction of aromatic, aliphatic and heterocyclic moieties at the 2-position of purine to improve its potency and selectivity. Specifically, these hybrids were substituted with different secondary amines to remarkably increase their activity beyond their normal scope. Synthesized compounds were well characterized by 1H and 13C NMR as well as mass spectroscopy. The newly synthesized compounds were screened for in vitro anticancer activities against 60 tumor cell lines panel assay. These results open up new opportunities for other biological activities.