Abstract Imidazole nucleus has been potential studied member from heterocyclic compound family. Imidazole and its derivatives showing good pharmacological activities against various diseases. Imidazole is the heterocyclic molecule which having the interesting physical and chemical properties, in the present article focus lies on analysis of these properties which in turn may be exploited for different pharmacological activities, like compounds having a 3,4,5-trimethoxyphenyl ring linked to either N-1 or C-4 position of the imidazole entity gave an interesting profile of cytotoxicity with specific activity against leukemia cell lines, combination of indole-imidazole compounds formed demonstrated substantial in vitro anti proliferative activities against cancer cell lines, effective substitutions are also made in the entity which resembles structures of various natural compounds whose anti cancerous activity has already been examined. The present review study highlighting pharmacological potential of the imidazole. In present study we have discussed compounds synthesized with imidazole moieties as their structural framework. Thus can say imidazole is a moiety which had been exploited in the past years for synthesizing various compounds having versatile pharmacological activities, and still it can be further utilized for future prospective against various pathological conditions and other uses.