Some small molecular compounds such as alkaloids have been shown to form bioactive complexes with metal ruthenium complexes. β-carboline is a kind of alkaloid widely found in nature in Marine organisms, cyanobacteria and mushrooms. Studies have shown that β-carboline compounds have biological activities.Two novel cyclometalated Ru(II) β-carboline complexes [Ru(dmb)2(NO2-Ph-βC)](PF6) (dmb = 4,4’-dimethyl-2,2’-bipyridine; NO2-Ph-βC = NO2-phenyl-9H-pyrido[3,4-b]indole; RuβC-5) and [Ru(bpy)2(NO2-Ph-βC)](PF6) (bpy = 2,2’-bipyridine; RuβC-6) were designed and synthesized. To explore the relationships between the structure and the biological activities of these two complexes, a series of assays including cell cycle arrest and apoptosis were investigated in HeLa tumor cells.