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

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, Alireza Foroumadi*.

Journal Name: Letters in Drug Design & Discovery

Volume 14 , Issue 10 , 2017

Become EABM
Become Reviewer

Graphical Abstract:


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.

Rights & PermissionsPrintExport Cite as


Article Details

VOLUME: 14
ISSUE: 10
Year: 2017
Page: [1138 - 1144]
Pages: 7
DOI: 10.2174/1570180814666170127164759
Price: $58

Article Metrics

PDF: 22
HTML: 1