Benzothiazole-piperazine derivatives prepared previously, 1h and 1j are potential anticancer agents. Since the mutagenic and genotoxic properties of anticancer drugs compose an essential issue to be researched, this study is focused on the analysis of the mutagenicity and genotoxicity of these molecules. The mutagenicity of 1h and 1j were determined by Ames test performed on Salmonella TA98 and TA100 strains. Sample 1j was mutagenic on TA98 bacterial strain. However, compound 1h was not mutagenic in bacterial strains TA98 and TA100 with and without S9 activation. The genotoxicity of 1h was evaluated by the chromosomal aberration assay on human lymphocytes. Compound 1h was also not genotoxic in human lymphocytes in vitro. All results revealed that, 1h was not mutagenic in the two Salmonella strains tested and was not genotoxic in chromosomal aberration assay. Therefore, results demonstrate that the described molecule is promising as a new anticancer drug without mutagenicity. Also, after performing Ames test with other recommended bacterial strains and in vivo experiments can be used safely for the development of new structures exhibiting anticancer activities.