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

[ Vol. 14 , Issue. 10 ]

Author(s):

Zahra Rezaei, Setareh Moghimi, Rezvan Javaheri, Mehdi Asadi, Mohammad Mahdavi, Shabnam Shabani, Najmeh Edraki, Omidreza Firuzi, Maliheh Safavi, Mohsen Amini, Ali Asadipour, Elnaz Zeinalzadeh, Loghman Firoozpour and Alireza Foroumadi*   Pages 1138 - 1144 ( 7 )

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.

Keywords:

Cancer, anticancer agents, 1, 3, 4-thiadiazole, phthalimide, anticancer agents, treatment.

Affiliation:

Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Drug Design & Development Research Center, Tehran University of Medical Sciences, Tehran, Department of Pharmaceutical Sciences, Islamic Azad University, Tehran 19395, Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Medicinal & Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Medicinal & Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Department of Biotechnology, Iranian Research Organization for Science and Technology, Tehran 33535-111, Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Department of Medicinal Chemistry, Faculty of Pharmacy and Neuroscience Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Drug Design & Development Research Center, Tehran University of Medical Sciences, Tehran, Drug Design & Development Research Center, Tehran University of Medical Sciences, Tehran, Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran

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