© 2014, Hacettepe University, Faculty of Pharmacy. All rights reserved.Bladder cancer is the third most common cancer in the world. Exposure to several compounds is related to bladder cancer occurrence and alkylanilines are the most anticipated chemicals that may cause this type of cancer. Humans are ubiquitously exposed to alkylanilines from cigarette smoking and use of permanent hair dyes. Exposure has been documented in humans based on hemoglobin adducts. Hemoglobin adduct formation was suspected to lead bladder cancer as well as cancers of liver, nasal cavity and subcutaneous tissue in rodents. Besides, alkylanilines were shown to cause DNA adducts in vivo and DNA adduct formation is a byproduct of metabolic activation. These compounds and their metabolites (particularly 3,5-dimethylaminophenol) were also demonstrated to have mutagenic and genotoxic effects. 3,5-dimethylaniline was shown to have the highest carcinogenic binding index (CBI) among other alkylanilines in mice and was classified as a moderate carcinogen in rodents. This review will focus on different alkylanilines and their toxic effects.