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

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

Volume: 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*

Affiliation:

• Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran,Iran

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

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.

Cite this article as:

Rezaei Zahra, Moghimi Setareh , Javaheri Rezvan, Asadi Mehdi, Mahdavi Mohammad, Shabani Shabnam, Edraki Najmeh, Firuzi Omidreza, Safavi Maliheh, Amini Mohsen, Asadipour Ali, Zeinalzadeh Elnaz , Firoozpour Loghman and Foroumadi Alireza*, Synthesis and Biological Evaluation of 1,3,4-Thiadiazole Linked Phthalimide Derivatives as Anticancer Agents, Letters in Drug Design & Discovery 2017; 14 (10) . https://dx.doi.org/10.2174/1570180814666170127164759

DOI https://dx.doi.org/10.2174/1570180814666170127164759	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X