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This book reported the literature survey of the chemistry of 2-cyanomethylbenzothiazole including the activity Syntheses and their synthetic importance. Furthermore, the obtained results were discussed, 41 novel compounds were synthesized, the synthetic mechanisms were investigated and compounds were established by elemental analysis and spectral data. The UV spectra of azo dyes provide additional evidence that such compounds have the hydrazone structure rather than the other structures. The newly synthesized compounds were screened for their antioxidant assay (ABTS method) and cytotoxicity activities against four different cell lines. Some of the compounds exhibited the promising activities. Finally, the experimental methods were included.