۴-Halo-N-(۵-(trifluoromethyl)-۱,۳,۴-thiadiazol-۲-yl)benzamide and Benzothioamide Derivatives: Synthesis and in vitro Anticancer Assessment

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 ۱,۳,۴-thiadiazole-based compounds were synthesized and evaluated for anti-cancer properties in vitro. The synthesis of ۵-(Trifluoromethyl)-۱,۳,۴-thiadiazol-۲-amine (۳) was carried out via solvent-free conditions and consequently, benzamide (۴a-۴f) and benzothioamide (۵a-۵f) derivatives bearing halogen moieties  (Cl, F) were synthesized. MTT assay was applied for in vitro cytotoxicity assessment against three cancerous cell lines consist of PC۳ (Prostate cancer), HT-۲۹ (Colon cancer), and SKNMC (Neuroblastoma). All tested derivatives exhibited equal or more (IC۵۰ = ۳-۷ µM) cytotoxic activity than doxorubicin (IC۵۰ = ۷ µM) as a reference drug against PC۳ cell line. Chlorine containing benzamideas well as benzothioamide derivatives (IC۵۰ = ۱۴-۳۶ µM) were also exerted a higher cytotoxic activity against SKNMC cell line compared to doxorubicin (IC۵۰ = ۴۰ µM).

کلیدواژه ها:

Synthesis ، ۱ ، ۳ ، ۴-Thiadiazole ، Anticancer ، MTT assay