University of Tehran Journal of Sciences, Islamic Republic of Iran 1016-1104 34 2 2023 06 01 Synthesis, Biological and Docking Studies of Thiadiazole Amide Derivatives Containing Anthranilic Acid 119 127 92628 10.22059/jsciences.2023.350957.1007765 EN Farshid Hassanzadeh Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Islamic Republic of Iran Elham Jafari Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Islamic Republic of Iran Mahshid Farzan Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Islamic Republic of Iran Hojjat Sadeghi-aliabadi Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Islamic Republic of Iran Journal Article 2022 11 09 Cancer has been become threatening the health and life of humans. Therefore, attempt to discovery more effective anticancer agents continue. Thiadiazole derivatives have been shown remarkable effects among chemotherapeutic agents. In this study, hybrid molecules containing thiadiazole amide derivatives -aromatic amines (anthranilic acid and 2, 5 dichloro aniline) were synthesized in multi-step reactions including N-amidation  and S-alkylation of thiadiazole. Synthesized compounds were assayed by MTT test against three cell lines. Molecular docking was performed on Src tyrosine kinases. Compounds <strong>5a</strong>, <strong>5b</strong> and <strong>8</strong> rendered remarkable cytotoxic properties on HeLa with IC₅₀‹60 µM. Compound <strong>5b</strong> showed significant cytotoxic effect on both cancer cell lines compared to other tested derivatives. Compound <strong>5</strong><strong>a</strong> with ΔG = -8.05kcal/mol was the best compound among  docked compounds.The results revealed that the quiddity of the amide  substitution  has a definitive role in the cytotoxic activity. https://jsciences.ut.ac.ir/article_92628_f5673b10b009a0f35f5985e1d4d46e23.pdf