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2-[2-(4-Arylamino)-4-methylphenylaminothiazol-5-oyl]naphthalenes have been synthesized by the reaction of 2-bromoacetyl naphthalene and 1-aryl-3-(N,N¹-diarylamidino)thiourea in the presence of triethyl amine. The structures of the newly synthesized analogues have been confirmed by spectroscopic techniques. The in vitro antioxidant activity has been studied using DPPH assay and anticancer activity has been studied using MTT assay against cancer cells. In silico studies have been performed to predict the binding modes of the compounds with the cyclin-dependent kinase protein 6WUU. It is evident from the current results that all the synthesized compounds exhibit remarkable antioxidant and anticancer potential. [ABSTRACT FROM AUTHOR]