Figure 1
Rationale for the designing of benzimidazoles-imidazo[1,2-a]pyrazine hybrids32,33. Over the past years, benzimidazole derivatives have been widely studied for their antimalarial34, anticancer35, antiprotozoal36, anti-inflammatory, and analgesic37 activities. On the other hand, imidazo[1,2-a]pyrazine is also reported as cyclic nucleotide phosphodiesterase inhibitor38, anticancer39, anti-inflammatory40, antioxidant41, antimicrobial42, antiviral43, and antimalarial agents44. Thus, the designing of benzimidazole-imidazo[1,2-a]pyrazine hybrid ring system has been taken that provides new compounds related to various biological activities of benzimidazole and imidazopyrazine, in the hope that new anti-tumor agents might be discovered. Alicyclic substitution at NH of benzimidazole moiety can enhance the pharmacokinetic properties of the scaffold. By taking these perspectives into consideration, the lead molecule was designed. To explore the effect of substitution on cytotoxicity, a library of compounds was synthesized by modification of different substitution on phenyl ring and benzimidazole moiety (Fig. 1).
