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In recent years for the development of novel anticancer hybrids with two or more pharmacophores of bioactive scaffolds to produce a single molecule by blending or linking has emerged as a simple strategy by providing an effective control on malignant process with improved biological potential. In this view, Sesamol being an active scaffold with important biological activities was modified and linked with various substitutions to afford thiazolidin-4-one derivatives. Herein, we report the synthesis, characterization of around twenty one compounds and their evaluation for antioxidant and anticancer potentials. The structures of these compounds were established by IR, 1H NMR, 13C NMR, and Mass. The compounds 1–15 were evaluated for in vitro cytotoxicity against three human lung cancer cell lines (A549, MCF-7 and HeLa), respectively. In preliminary MTT [3-(4,5- dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] cytotoxicity studies compounds 9 and 12 were found most effective. In A549 cancer cells the CTC50 (50% of cytotoxicity inhibition) were observed at 84.27 ± 2.7 & 91.98 ± 4.2 µg/ml, respectively. Moreover, in MCF-7 and HeLa cells the CTC50 values were observed at 174.3 ± 4 4.1, 69.15 ± 3.4 and 42.90 ± 3.5, 180.77 ± 4.6 µg/ml, respectively. Compounds 9 and 12 also exhibited best DNA damage activity via cell apoptosis when screened against Human breast cancer cell lines A549 and MCF-7 when compared to standard doxorubicin. In this study, Compounds 1, 9, 11 and 12 (at concentration 100 mg/kg/body wt.) were selected for in vivo anticancer activity against Dalton’s Lymphoma Ascites bearing mice. Among the tested compounds all has shown modest antitumor activity and merited anti-cancer activity due to its cytotoxic properties when compared with standard methotrexate.