4-Halo-N-(5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl)benzamide and Benzothioamide Derivatives: Synthesis and in vitro Anticancer Assessment

Document Type : Research Article


1 Pharmaceutical Sciences Research Center, Health Institute, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, I.R. IRAN

2 Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, I.R. IRAN


Cancer is a lethal disorder that has caused a serious threat to human health and nowadays there is a crucial need for the development of novel anticancer agents. A new series of 1,3,4-thiadiazole-based compounds were synthesized and evaluated for anti-cancer properties in vitro. The synthesis of 5-(Trifluoromethyl)-1,3,4-thiadiazol-2-amine (3) was carried out via solvent-free conditions and consequently, benzamide (4a-4f) and benzothioamide (5a-5f) derivatives bearing halogen moieties  (Cl, F) were synthesized. MTT assay was applied for in vitro cytotoxicity assessment against three cancerous cell lines consist of PC3 (Prostate cancer), HT-29 (Colon cancer), and SKNMC (Neuroblastoma). All tested derivatives exhibited equal or more (IC50 = 3-7 µM) cytotoxic activity than doxorubicin (IC50 = 7 µM) as a reference drug against PC3 cell line. Chlorine containing benzamideas well as benzothioamide derivatives (IC50 = 14-36 µM) were also exerted a higher cytotoxic activity against SKNMC cell line compared to doxorubicin (IC50 = 40 µM).


Main Subjects

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