A　series　of　1,3-disubstituted　imidazolium　salts　were　synthesized　through　a　convenient　synthetic　approach　based　on　the　reaction　of　1,4-diazabuta-1,3-dienes　with　HClO4.　Their　antitumor　activity　was　evaluated　in　vitro　against　a　number　of　human　cancer　cells.　1,3-Bis[(3,5-bis(trifluoromethyl)phenyl]imidazolium　perchlorate　turned　out　to　be　the　most　active　against　A549　and　MCF-7　cancer　cell　lines　with　IC50　values　of　5.24　and　4.21　mu　M,　respectively.　The　results　of　structure-activity　relationship　study　indicated　that　substituents　on　the　imidazole　derivatives　play　an　important　role　in　their　cytotoxic　activities.　Finally,　molecular　docking　of　some　tested　compounds　was　carried　out　in　order　to　investigate　their　binding　pattern　with　the　CDK2.