title: Discovery of 2-phenyl-N-(5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl)acetamide derivatives as apoptosis inducers via the caspase pathway with potential anticancer activity.
abstract: In the current research of medicinal chemistry, apoptosis induction is one of the novel strategies for the development and discovery of novel anticancer therapeutics. In the present study, a new series of 1,3,4-thiadiazole derivatives (4a-4p) were synthesized and their in vitro anticancer activities were evaluated against three cancer cell lines: PC3 (prostate cancer), MCF7 (breast cancer), and SKNMC (neuroblastoma). These cell lines were utilized in MTT assays and the obtained results were compared to doxorubicin. Apoptosis induction was also investigated through exploration of the activation of caspases 3, 8, and 9. According to the obtained results, compounds 4b (3-Cl) and 4c (4-Cl) demonstrated the best caspase activation. In fact, compounds 4b and 4c enhanced the activity of caspases 3 and 9 in the MCF7 cell line.
authors.affiliation: Faculty of Pharmacy, Department of Pharmacology, Toxicology and Medical Services, Kermanshah University of Medical Sciences, Kermanshah, Iran.
authors.forename: Leila
authors.initials: L
authors.lastname: Hosseinzadeh
authors.forename: Amanc
authors.initials: A
authors.lastname: Khorand
authors.forename: Alireza
authors.initials: A
authors.lastname: Aliabadi
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D020169:Caspases / Q000378:metabolism*; D002470:Cell Survival / Q000187:drug effects; D055808:Drug Discovery; D004789:Enzyme Activation; D020536:Enzyme Activators / Q000138:chemical synthesis / Q000494:pharmacology*; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D061986:MCF-7 Cells; D008297:Male; D015394:Molecular Structure; D009369:Neoplasms / Q000201:enzymology* / Q000473:pathology; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D020536:Enzyme Activators; D013830:Thiadiazoles; C058949:1,3,4-thiadiazole; D020169:Caspases
keywords: 1,3,4-Thiadiazole; Anticancer; Apoptosis; Caspase enzymes; Synthesis