4-halo-n-(5-(trifluoromethyl)-1,3,4-thiadiazol-2-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 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 benzamide as 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).