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Synthesis and Biological Evaluation of 1,3,4-Thiadiazole Linked Phthalimide Derivatives As Anticancer Agents Publisher



Rezaeia Z1 ; Moghimi S2 ; Javaheri R3 ; Asadi M1 ; Mahdavi M4 ; Shabani S5 ; Edraki N6 ; Firuzi O6 ; Safavi M7 ; Aminia M1 ; Asadipour A8 ; Zeinalzadeh E2 ; Firoozpour L2 ; Foroumadi A5
Authors

Source: Letters in Drug Design and Discovery Published:2017


Abstract

Background: Due to the importance of 1,3,4-thiadiazoles and phthalimides in anticancer agents, a novel series of 1,3,4-thiadiazole-phthalimide system have been synthesized and evaluated in vitro against HT-29 and MCF-7 human cancer cell lines. Methods: The target compounds were prepared through four-step reaction and their cytotoxicities were evaluated by MTT assay. Results: The results showed that 4-nitrobenzoyl moiety containing derivatives are the most potent ones. The morphological evaluation also indicated that these compounds are apoptotic inducers. Conclusion: 4-Nitro-N-(5-((3-(1,3-dioxoisoindolin-2-yl)propyl)thio)-1,3,4-thiadiazol-2-yl)benzamide (8m) exhibits the best inhibitory effect against HT-29 and MCF-7 cell lines with IC50 values of 23.83 and 27.21 μM, respectively. © 2017 Bentham Science Publishers.
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